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Onion: Health Benefits and Medical Uses ( acts as blood thinner)

August 6, 2013 2:56 pm / Leave a comment

Onion is a commonly known plant. The part used is the bulb, which grows underground. It is an essential part of our kitchen herbs and spices. Onion is used in lots of recipes all over the world particularly in South Asia. It is both herb and vegetable used in all seasons. It has been part of many herbal preparations particularly sexual medicines since ages due to its medical properties. Apart from the chemistry of onion, it has dry-warm characteristics, which are used to treat various ailments. It is a boon for those having wet-cold constitutions. Many diseases associated with wet-cold group can be treated with onion. In homeopathy it comes under the name Allium Cepa and is used for a multitude of symptoms. Following are some of the common uses: –

Asthma
Cholera
It is an excellent first aid for cholera. In most cases, a teaspoonful of onion juice can give immediate relief.
Diabetes Mellitus
Very useful in lowering the level of blood sugar.

– See more at:

http://www.homeopathy.com.pk/kitchen-herbs/onion-health-benefits-medical-uses.php

http://www.homeopathy.com.pk/kitchen-herbs/onion-health-benefits-medical-uses.php#sthash.vmiEqWJl.dpuf

webmd info

Onion is a plant. The bulb (rounded underground part) of the onion is used to make medicine.

Onion is used for treating digestion problems including loss of appetite, upsetstomach, and gallbladder disorders; for treating heart and blood vessel problems including chest pain (angina) and high blood pressure; and for preventing “hardening of the arteries” (atherosclerosis). It is also used for treating sore mouth and throat,whooping cough, bronchitis, asthma, dehydration, intestinal gas, parasitic worms, and diabetes. Some people use it as a diuretic to increase urine output.

Onion is applied directly to the skin for insect bites, wounds, light burns, boils, warts, and bruises.

In foods, onion is used in many recipes.

In manufacturing, the oil is used to flavor foods.

How does it work?

Onion might help reduce cholesterol levels, a risk factor for hardening of the arteries. There is some evidence that onion might also reduce lung tightness in people with asthma.

MEDICINAL QUALITIES OF ONION

Research shows that onions may help guard against many chronic diseases. That’s probably because onions contain generous amounts of the flavonoid quercetin. Studies have shown that quercetin protects against cataracts, cardiovascular disease, and cancer. In addition, onions contain a variety of other naturally occurring chemicals known as organosulfur com-pounds that have been linked to lowering blood pressure and cholesterol levels.7Onions contain 25 active compounds that appear to inhibit the growth of cancerous cells alliin being the main constituent. Onion has been found to help combat heart disease, inhibit strokes, lower blood pressure and cholesterol, and stimulate the immune system. The potassium salts and the flavonoides that are present perform an anti-inflammatory action. The essential oil is an expectorant, antiseptic, antifungal, anticoagulant, high-blood pressure, antithelmitic, balsamic, rubefciant, and has analgesic properties

In investigating the use of onion in medicinal terms, the onion is found to be a remedy for conditions with symptoms like those which are caused by exposure to onions, such as watering eyes, and a burning and running nose. When looking at the symptoms of cold, it is ironic that we would treat this ailment with an almost like-with-like therapy. Alliums are antibacterial and anti-fungal, so they can help ward off colds and treat colds with sinus congestion that shifts from side to side in the head. Onion will relieve coughs that cause a ripping or tearing pain in the throat or a cough that is merely an irritating dry tickle. The watery and inflamed eyes due to sinus con-gestion and hay fever will be greatly relieved with onion.

The onions ability to relieve congestions especially in the lungs and bronchial tract, is hard to believe until you have actually witnessed the results. The drawing of infection, congestion and colds out of the ear is also remarkable.

The onion will relieve stomach upset and other gastrointestinal disorders and it will also strengthen the appetite.

Onions help prevent thrombosis and reduce hypertension, according to the American Heart Association. 8 The natural constituents of yellow or white onions can “…raise HDL cholesterol by 30% over time”, according to Dr. Victor Gurewich of Tufts University.9

The onion is being used for compresses to be applied to the skin for acne, arthritis, and congestion, and used internally for worms. The onion is also known for its diuretic properties.

There have been cases in which the onion has been proven to be so effective as an antiviral that a cut piece of onion placed in a closed off room will prevent the person in the room to be safe from viruses.

Onion will relieve headache centered behind the forehead; earache in children and adults; stuffed up nose with discharge that makes nostrils and upper lip sore or stuffed up nose with discharge from the alternate nostril; toothache, especially in the molar area or the shifting from side to side or from one tooth to another; hoarseness and the early stages of laryngitis; abdominal colic in babies.

Keeping cooler rooms in the home, and getting plenty of fresh air may prevent the symptoms of a stuffy nose and hoarseness

Never mind the tears they bring on—onions are an ace ally in your fight against disease. A prized member of the lily family, they lavish you with health benefits while adding oodles of taste to your food.

A quick glimpse at their incredible health benefits:

The phytochemicals in onions improve the working of Vitamin C in the body, thus gifting you with improved immunity.
Onions contain chromium, which assists in regulating blood sugar.
For centuries, onions have been used to reduce inflammation and heal infections.
Do you enjoy sliced onions with your food? If yes, rejoice! Raw onion encourages the production of good cholesterol (HDL), thus keeping your heart healthy.
A powerful compound called quercetin in onions is known to play a significant role in preventing cancer.
Got bitten by a honeybee? Apply onion juice on the area for immediate relief from the pain and burning sensation.
Onions scavenge free radicals, thereby reducing your risk of developing gastric ulcers.
Those bright green tops of green onions are rich in Vitamin A, so do use them often.

My favorite way to enjoy onions is to slice them really thin, squeeze some lemon juice on top and add a little salt. Sprinkling a few freshly washed cilantro leaves adds fragrance and flavor to this simple, quick salad, without which no dinner of mine is complete.

Onion cells from tammi-1990

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The rind of the Vrikshamla (Garcinia/Garcinia indica) fruit contains an active component called hydroxycitric acid (HCA), which supports normal fat and carbohydrate metabolism, a healthy appetite level and optimum body weight

August 5, 2013 7:00 am / 56 Comments on The rind of the Vrikshamla (Garcinia/Garcinia indica) fruit contains an active component called hydroxycitric acid (HCA), which supports normal fat and carbohydrate metabolism, a healthy appetite level and optimum body weight


Kokum fruits, seeds, pulp and rinds.jpg

The rind of the Vrikshamla (Garcinia/Garcinia indica) fruit contains an active component called hydroxycitric acid (HCA), which supports normal fat and carbohydrate metabolism, a healthy appetite level and optimum body weight. The Department of Physiology researchers at the Georgetown University Medical Center in Washington DC, called Vrikshamla a safe, natural supplement for normal weight support. In an eight-week study of 60 volunteers, they reported Vrikshamla’s effectiveness in supporting normal weight, cholesterol, triglyceride and serum lipid levels.

hydroxycitric acid (HCA)

Vrikshamla grows in India the evergreen forests of the Western Ghats, the Southern Konkan region and in Goa. It is also cultivated in the Southern districts of Maharashtra and on the lower slopes of the Nilgiris mountains.

Active constituents:

The active constituent in this herb, HCA, helps weight loss by promoting normal appetite levels and by reducing the body’s ability to form adipose (fatty) tissue. HCA also reduces blood lipid levels and naturally lowers cholesterol. Other useful phytochemicals in Vrikshamla are garcinol, isogarcinol, xanthochymol and isoxanthochymol.

Herb Functions:

Weight management: The herb known to slow down the body’s ability to store fat, potentially enabling more fat from foods to pass through the body without being stored. Additionally, HCA blocks the production and storage of fat and cholesterol when calorie consumption exceeds healthy levels. The herb is also known to reduce blood lipid levels and to naturally lower cholesterol.

read at

http://www.himalayahealthcare.com/products/pharmaceuticals/vrikshamla.htm

Garcinia indica, a plant in the mangosteen family (Clusiaceae), commonly known askokum, punar puli (tulu language), is a fruit-bearing tree that has culinary, pharmaceutical, and industrial uses.

The genus Garcinia, belonging to the family Clusiaceae, includes about 200 species found in the Old World tropics, mostly in Asia and Africa. Garcinia indica is indigenous to theWestern Ghats region of India located along the western coast of the country. Of the 35 species found in India, 17 are endemic. Of these, seven are endemic to the Western Ghats, six in the Andaman and Nicobar Islands and four in the northeastern region of India.

Garcinia indica is found in forest lands, riversides and wastelands. These plants preferevergreen forests, but sometimes they also thrive in areas with relatively low rainfall. It is also cultivated on a small scale. It does not require irrigation, spraying of pesticides or fertilizers.

Garcinia indica is known by various names across India, including aamsol, aamsul, bindin, biran, bhirand,bhrinda, brinda, bin’na, kokum (alternate spellings kokam and cocum), katambi, looikya, sour apple, panarpuli, ratamba, thekera (in Assam) and many others.

The dried skin of kokum fruits

The outer cover of fruit is dried in the sun to get aamsul or kokam. It is used as a slightly sour spice in recipes from Maharashtra. Kokum yields a peculiar flavour and blackish red colour. It is a preferred substitute for tamarind in curries and other dishes from the Konkanregion. It is also used in cuisine from Gujarat, where it is frequently used to add flavor and tartness to dal (lentil soup) for flavor balance, and parts of South India.

The vessel on the left contains syrup which is obtained from the vessel containing kokum rinds, on the right. The syrup is used to make kokum sherbet

Kokum squash or kokum concentrate is used in preparing a drink (sherbet) which is bright red in colour. Kokum sherbet improves digestion and cools the body during summers^{[citation needed]}.

Further, the extract/ concentrate of this fruit is called aagal in Konkani and Marathi. It is to added during the preparation of solkadhi, along with coconut milk.

Industrial uses

The seed of Garcinia indica contains 23–26% oil, which remains solid at room temperature. It is used in the preparation of confectionery, medicines and cosmetics.

Recently, industries have started extracting hydroxycitric acid (HCA) from the rind of the fruit.^{[citation needed]}

The tree is ornamental, with a dense canopy of green leaves and red-tinged, tender, young leaves. The oily extract called kokum tel is used in foot massage.

Vivimed Acquires A US FDA Approved Formulation Manufacturing Facility

August 5, 2013 5:06 am / 1 Comment on Vivimed Acquires A US FDA Approved Formulation Manufacturing Facility

Managing Director and CEO Santosh Varalwar, vivimed labs ltd

Vivimed Labs Ltd, established in 1989, is a diversified global company with a unique portfolio of products in Specialty Chemicals and Pharmaceuticals. Vivimed has gradually increased its portfolio of offerings through product innovations at its Research & Development Center. Some of its reputed clientele includes Unilever, P&G, L’Oreal, ISP, Novartis, Merck, Cipla, Astra Zeneca, BDF, AVON and others. The Product offerings comprises Hair care, Skincare, Oral Care, Antimicrobials & Preservatives, Photo Imaging Chemicals & Photo Chromic, Specialized Formulations such as Opthalamic, Anti Ulcer, Antehelminth and other health care segments

1 aug 2013

Vivimed Labs Ltd., manufacturer of specialty chemicals and pharmaceuticals, announced the signing of an agreement to acquire Actavis Pharma Manufacturing Pvt. Ltd.’s solid oral dosage facility in Alathur in Tamil Nadu for an aggregate consideration of Rs.122 crore.

The facility is being acquired from its parent Actavis Holding Asia B.V., an affiliate of Actavis Inc., a leading global general and specialty pharmaceutical company.

read at

http://pharmadeals.pharmaintellect.com/2013/08/vivimed-acquires-us-fda-approved.html?utm_source=feedburner&utm_medium=email&utm_campaign=Feed%3A+Pharmainvest+%28PharmaInvest%29

Flow synthesis for Novartis anticancer drug, Gleevec, Imatinib

August 5, 2013 4:24 am / 4 Comments on Flow synthesis for Novartis anticancer drug, Gleevec, Imatinib

The flow-based route required minimal manual intervention and was achieved despite poor solubility of many reaction components

21 January 2013Michael Parkin

http://www.rsc.org/chemistryworld/2013/01/flow-synthesis-anticancer-drug

UK chemists have used a combination of flow chemistry methods with solid-supported scavengers and reagents to synthesise the active pharmaceutical ingredient, imatinib, of the anticancer drug Gleevec. The method avoids the need for any manual handling of intermediates and allows the drug to be synthesised in high purity in less than a day.

Gleevec, developed by Novartis, is a tyrosine kinase inhibitor used for the treatment of chronic myeloid leukaemia and gastrointestinal stromal tumours.

READ ALL AT

http://www.rsc.org/chemistryworld/2013/01/flow-synthesis-anticancer-drug



IMATINIB

CREDIT

http://www.veomed.com/va041542042010

‘Wrapping’ Gleevec Fights Drug-Resistant Cancer, Study Shows

http://www.sciencedaily.com/releases/2007/05/070501115127.htm

The anti-cancer drug Gleevec® is far more effective against a drug-resistant strain of cancer when the drug wraps the target with a molecular bandage that seals out water from a critical area. This image shows the bandage (black box) on the modified version of the drug, WBZ-7. (Credit: Image courtesy of Rice University)

A new study in Cancer Research finds that the anti-cancer drug Gleevec® is far more effective against a drug-resistant strain of cancer when the drug wraps the target with a molecular bandage that seals out water from a critical area.

FDA Grants Priority Review To New Drug Application For MNK-795

August 5, 2013 3:13 am / 3 Comments on FDA Grants Priority Review To New Drug Application For MNK-795

FDA Grants Priority Review To New Drug Application For MNK-795 Submitted By Depomed Licensee Mallinckrodt

Controlled Substance Analgesic Combination Product Uses Depomed’s Proprietary Acuform® Technology

NEWARK, Calif., July 29, 2013 /PRNewswire/ — Depomed, Inc. (NASDAQ:DEPO) announced today that the U. S. Food and Drug Administration (FDA) has accepted for filing a New Drug Application (NDA) from Mallinckrodt (NYSE: MNK) for MNK-795. MNK-795 is a controlled-release oral formulation of oxycodone and acetaminophen that has been studied for the management of moderate to severe acute pain where the use of an opioid analgesic is appropriate. MNK-795 is formulated with Depomed’s Acuform® drug delivery technology.

http://www.pharmalive.com/fda-grants-priority-review-to-new-drug-application-for-mnk-795

Regulatory update: albiglutide US PDUFA date extended by three months

August 4, 2013 3:24 am / 2 Comments on Regulatory update: albiglutide US PDUFA date extended by three months

albiglutide,

Friday 2 August 2013, London UK

GlaxoSmithKline plc (LSE:GSK) today announced that the US Prescription Drug User Fee Act (PDUFA) goal date for albiglutide, an investigational once-weekly treatment for adult patients with type 2 diabetes, has been extended by three months to 15 April 2014 to provide time for a full review of information submitted by GSK in response to the Food and Drug Administration’s requests.

http://www.pharmalive.com/fda-delays-approval-decision-for-gsk-s-albiglutide

Albiglutide is a glucagon-like peptide-1 agonist (GLP-1 agonist) drug under investigation by GlaxoSmithKline for treatment oftype 2 diabetes. It is a dipeptidyl peptidase-4-resistant glucagon-like peptide-1 dimer fused to human albumin.

Albiglutide has a half-life of four to seven days, which is considerably longer than the other two GLP-1 analogs approved for market use, exenatide (Byetta) and liraglutide (Victoza). GLP-1 drugs are currently only available for subcutaneous administration on a daily basis, so a GLP-1 drug with a longer half-life is desirable. Such a drug would only need to be injected biweekly or weekly instead of daily, reducing the discomfort and inconvenience of GLP-1 administration considerably.

It has not yet been determined whether albiglutide is as effective an antidiabetic agent as GLP-1 drugs currently on the market, and final data remain to be published regarding the incidence of adverse effects related to the drug. To evaluate the efficacy and safety of the drug, albiglutide is undergoing eight Phase III clinical trials. Four of these trials should report useful data by end 2010

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DENDRIMER: A NOVEL SYSTEM IN PHARMACEUTICALS | EUREKAMOMENTS IN ORGANIC CHEMISTRY

August 3, 2013 8:52 am / 3 Comments on DENDRIMER: A NOVEL SYSTEM IN PHARMACEUTICALS | EUREKAMOMENTS IN ORGANIC CHEMISTRY

DENDRIMER: A NOVEL SYSTEM IN PHARMACEUTICALS | EUREKAMOMENTS IN ORGANIC CHEMISTRY.

FDA has granted tentative approval to India-based Strides Arcolab’s HIV drug emtricitabine and tenofovir disoproxil fumarate tablets, 200 mg/300 mg.

August 3, 2013 6:45 am / 3 Comments on FDA has granted tentative approval to India-based Strides Arcolab’s HIV drug emtricitabine and tenofovir disoproxil fumarate tablets, 200 mg/300 mg.

http://www.stridesarco.com/

chief executive and vice chairman Arun Kumar –Strides arcolab

Deepak Vaidya, chaiman

Headquartered in India, Strides Arcolab is a pharmaceutical company with a key focus on the development and manufacture of IP-led niche products, particularly sterile injectables. It is among the world’s largest manufacturers of soft gelatin capsules. With 14 world-class manufacturing facilities, an innovative R&D hub and a marketing network in 70 countries, Strides is well positioned to meet the demands of the global pharmaceutical industry and has partnered with several of the world’s leading pharmaceutical companies.

2 August 2013

Strides Arcolab’s HIV drug, which is generic version of Gilead Sciences’ Truvada, gets tentative approval from the US FDA.

Tentative approval implies that the drug has met all standards but cannot be marketed in the US due to existing patent protections Good news for HIV AIDS patients

FDA has granted tentative approval to India-based Strides Arcolab’s HIV drug emtricitabine and tenofovir disoproxil fumarate tablets, 200 mg/300 mg. The drug is a generic version of Truvada, 200 mg/300 mg tablets, which is manufactured by Gilead Sciences.

The product is indicated for use in combination with other antiretroviral agents for the treatment of human immunodeficiency virus (HIV)-1

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EMTRICITABINE

credit-chemdrug

The selective tosylation of L-gulose with tosyl chloride in pyridine, followed by complete acetylation with acetic anhydride gives tetraacetyl-6-O-tosyl-L-gulose (II), which is treated with HBr in AcOH to yield the bromo derivative (III ). The reaction of (III) with potassium O-ethylxanthate in refluxing acetone, followed by deacetylation with NH4OH in methanol affords 1,6-thioanhydro-L-gulopyranose (IV). The selective oxidative cleavage of (IV) by means of NaIO4 , followed by reduction with NaBH4 and protection of the resulting diol with acetone and TsOH provides the acetonide (V), which is silylated at the primary OH group with TBDMS-Cl giving the silyl ether (VI). Elimination of the acetonide group with TsOH in methanol yields the diol (VII), which is cleaved with Pb (OAc) 4 and oxidized with PDC in DMF to afford the carboxylic acid (VIII). The treatment of (VII) with Pb (OAc) 4/pyridine in THF furnishes the diacetate (IX), which is condensed with N4-acetyl-5-fluoro-O-(trimethylsilyl) cytosine (X) by means of TBDMS-OTf in dichloromethane yielding a mixture of the desired (-) (2R, 5S) – isomer (XI) along with its (+) – (2R, 5R)-isomer that is separated by column chromatography. Finally, deacetylation of (XI) with ammonia in methanol, followed by desilylation with TBAF in THF afforded the target compound.

Jeong, LS; et al.; Asymmetric synthesis and biological evaluation of beta-L-(2R, 5S) – and alpha-L-(2R, 5R) -1, 3-oxathiolane-pyrimidine and-purine nucleosides as potential anti- HIV agents. J Med Chem 1993, 36, 2, 181

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TENOFOVIR

DONEPEZIL SYNTHESIS

August 2, 2013 3:25 am / 3 Comments on DONEPEZIL SYNTHESIS

Donepezil, marketed under the trade name Aricept by its developer Eisai and partnerPfizer, is a centrally acting reversible acetylcholinesterase inhibitor. Its main therapeutic use is in the palliative treatment of Alzheimer’s disease.Common side effects include gastrointestinal upset. It has an oral bioavailability of 100% and easily crosses the blood–brain barrier. Because it has a biological half-life of about 70 hours, it can be taken once a day.

Currently, no definitive proof shows the use of donepezil or other similar agents alters the course or progression of Alzheimer’s disease (AD). However, 6 to 12-month controlled studies have shown modest benefits in cognition and/or behavior.Pilot studies have reported donepezil therapy may potentially have effects on markers of disease progression, such as hippocampal volume. Therefore, many neurologists, psychiatrists, and primary-care physicians use donepezil in patients with Alzheimer’s disease. In 2005, the UK National Institute for Clinical Excellence (NICE) withdrew its recommendation for use of the drug for mild-to-moderate AD, on the basis of no significant improvement in functional outcome, quality of life, or behavioral symptoms. However, NICE revised its guidelines to suggest donepezil be used in moderate-stage patients for whom the evidence is strongest.

While the drug is currently indicated for mild to moderate Alzheimer’s, evidence from two clinical trials also indicates it may be effective for moderate to severe disease. An example of this is a Karolinska Institute paper published in The Lancet in early 2006, which states donepezil improves cognitive function even in patients with severe AD symptoms. In Oct. 2006 the U.S. Food and Drug Administration also approved Aricept for treatment of severe dementia.

【通用名】 Donepezil hydrochloride, BNAG, E-2020, Eranz, Memorit, Memac, Aricept
【化学名】 (?-1-Benzyl-4-(5,6-dimethoxy-1-oxoindan-2-ylmethyl)piperidine hydrochloride; (?-2-(1-Benzylpiperidin-4-ylmethyl)-5,6-dimethoxyindan-1-one hydrochloride
【CAS登记号】 120011-70-3, 123958-79-2 ([2-14C]-labeled), 142057-77-0 (deleted CAS), 120014-06-4 (free base)
【分子式】 C24-H29-N-O3.Cl-H
【分子量】 415.958
【化学活性】 Alzheimer’s Dementia, Treatment of , Analgesic and Anesthetic Drugs, Antimigraine Drugs, Attention Deficit Hyperactivity Disorder (ADHD), Treatment of, Autism, Treatment of, Cognition Disorders, Treatment of, Immunologic Neuromuscular Disorders, Treatment of, Migraine, Prophylactic Treatment of, Multiple Sclerosis, Agents for, Neurologic Drugs, Psychopharmacologic Drugs, Vascular Dementia, Treatment of, Acetylcholinesterase Inhibitors
【开发阶段】 Launched-1997
【研究机构】 Eisai (Originator), National Institute of Mental Health (Not Determined), Bracco (Licensee), Pfizer (Licensee)

Donepezil inhibiting Torpedo californicaacetylcholinesterase. See Proteopedia 1eve.

Research leading to the development of donepezil began in 1983 at Eisai, and the first Phase I clinical trial took place in 1989. In 1996, Eisai received approval from the United States Food and Drug Administration (USFDA) for donepezil under the brand Aricept, which it co-marketed with Pfizer. As of 2011, Aricept was the world’s best-selling Alzheimer’s disease treatment. The first generic donepezil became available in November 2010 with the USFDA approval of a formulation prepared by Ranbaxy Labs. In April 2011 a second generic formulation, from Wockhardt, received tentative USFDA marketing approval


标题:	Cyclic amine cpd., its use and pharmaceutical compsns. comprising it
作者:	Sugimoto, H.; Tsuchiya, Y.; Higurashi, K.; Karibe, N.; Iimura, Y.; Sasaki, A.; Yamanashi, Y.; Ogura, H.; Araki, S.; Kosasa, T.; Kusota, A.; Kozasa, M.; Yamatsu, K. (Eisai Co., Ltd.)
来源:	AU 8818216; EP 0296560; EP 0673927; EP 0742207; JP 1989079151; JP 1998067739; US 4895841; US 5100901

合成路线图解说明:The condensation of 5,6-dimethoxy-1-indanone (I) with 1-benzylpiperidine-4-carboxaldehyde (II) by means of butyllithium and diisopropylamine in THF gives 1-benzyl-4-(5,6-dimethoxy-1-oxoindan-2-ylidenemethyl)piperidine (III), which is reduced with H2 over Pd/C in THF and treated with HCl in dichloromethane – ethyl acetate.


标题:	Synthesis of 1-benzyl-4-[(5,6-dimethoxy[2-14C]-1-indanon)-2-yl]methylpiperidine hydrochloride (E-2020-14C)
作者:	Sugimoto, H.; Mishima, M.; Iimura, Y.
来源:	J Label Compd Radiopharm 1989,27(7),835-9

合成路线图解说明:The condensation of 5,6-dimethoxy-1-indanone (I) with 1-benzylpiperidine-4-carboxaldehyde (II) by means of butyllithium and diisopropylamine in THF gives 1-benzyl-4-(5,6-dimethoxy-1-oxoindan-2-ylidenemethyl)piperidine (III), which is reduced with H2 over Pd/C in THF and treated with HCl in dichloromethane – ethyl acetate.



作者:	Casta馿r, J.; Prous, J.
来源:	Drugs Fut 1991,16(1),16

合成路线图解说明:The condensation of 5,6-dimethoxy-1-indanone (I) with 1-benzylpiperidine-4-carboxaldehyde (II) by means of butyllithium and diisopropylamine in THF gives 1-benzyl-4-(5,6-dimethoxy-1-oxoindan-2-ylidenemethyl)piperidine (III), which is reduced with H2 over Pd/C in THF and treated with HCl in dichloromethane – ethyl acetate.


标题:	Synthesis of 1-benzyl-4-[(5,[C-11]6-dimethoxy-1-oxoindan-2-yl)methyl]piperidine: A promising ligand for visualisation of acetylcholine esterase by PET
作者:	Santens, P.; DeReuck, J.; Dierckx, R.A.; Siegers, G.; Vermeirsch, H.; De Vos, F.
来源:	J Label Compd Radiopharm 2000,43(6),595

合成路线图解说明:11C-Labeled donepezil was prepared by methylation of 2-(1-benzylpiperidin-4-ylmethyl)-6-hydroxy-5-methoxyindan-1-one (I) with 11CH3I by means of tetrabutylammonium hydroxide in DMF.

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Drug treatment of alzheimers disease from Naser Tadvi

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Donepezil hydrochloride is a useful memory enhancer introduced by the Japanese pharmaceutical company Eisai. Its preparation was described in patent no. EP 296560. In this patent Donepezil was produced by reaction of 5,6-dimethoxy-1- indanone with 1 -benzyl-4-formylpiperidine in the presence of a strong base, such as lithium diisopropylamide followed by reduction of the double bond. According to this method, Donepezil was obtained (Scheme 1).Patent application WO 99/36405 describes another process for the synthesis of Donepezil. According to this patent, 2-alkoxycarbonyl-1-indanones are reacted with (4-pyridinyl) methyl halide moiety followed by hydrolysis and decarboxylation to give the 2-(4-pyridinyl)methyl-1-indanone derivative. This is followed by reaction with benzyl halides to obtain the corresponding quaternary ammonium salt, and followed by hydrogenation of the pyridine ring to obtain Donepezil (Scheme 2).Patent application WO 97/22584 describes the preparation of Donepezil by reaction of pyridine-4-carboxyaldehyde with malonic acid to give 3-(pyridin-4-yl)-2- propenoic acid, followed by hydrogenation of the double bond to give 3-(piperidin-4-yl)-2-propionic acid. Reaction of this intermediate with methyl chloroformate afforded 3-[N-(methyloxycarbonyl) piperidin-4-yl]propionic acid. This was followed by reaction with oxalyl chloride to give methyl 4-(2-chlorocarbonylethyl)piperidin-1-carboxylate. Reaction with 1,2-dimethoxybenzene in the presence of aluminum chloride afforded methyl 4-[3-(3,4-dimethoxyphenyl)-3-oxopropyl]piperidin-1 -carboxylate. Reaction with tetramethyldiaminomethane afforded 4-[2-(3,4-dimethoxybenzoyl)allyl] piperidin-1-carboxylate. Reaction with sulfuric acid afforded methyl 4-(5,6-dimethoxy-1-oxoindan-2-yl)methylpiperidin-1- carboxylate. This was followed by treatment with base to give 5,6-dimethoxy-2-(piperidin-4-ylmethyl) indan-1-one, then reaction with benzyl bromide afforded Donepezil (Scheme 3).

Patent application EP 711756 describes the preparation of Donepezil by reaction of 5,6-dimethoxy-1- indanone with pyridin-4-aldehyde to give 5,6-dimethoxy-2-(pyridin-4-yl)methylene indan-1-one. Reaction with benzyl bromide afforded 1-benzyl-4-(5,6-dimethoxyindan-1-on-2-ylidene)methylpyridinium bromide. Hydrogenation in the presence of platinum oxide afforded Donepezil (Scheme 4).

United States Patent 6844440

EP 1386607 A1

FDA Grants Priority Review To New Drug Application For MNK-795 Submitted By Depomed Licensee Mallinckrodt

August 1, 2013 1:05 pm / Leave a comment

FDA Grants Priority Review To New Drug Application For MNK-795 Submitted By Depomed Licensee Mallinckrodt

Controlled Substance Analgesic Combination Product Uses Depomed’s Proprietary Acuform® Technology

http://www.pharmalive.com/fda-grants-priority-review-to-new-drug-application-for-mnk-795

	Bosmolisib – N… on Bosmolisib
	Cenacitinib –… on Cenacitinib
	Emestedastat –… on Emestedastat
	Enrupatinib –… on Enrupatinib
	Evetifator – N… on Evetifator

Tag Archives: medicinal chemistry

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Active constituents:

Herb Functions:

Industrial uses

The tree is ornamental, with a dense canopy of green leaves and red-tinged, tender, young leaves. The oily extract called kokum tel is used in foot massage.

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‘Wrapping’ Gleevec Fights Drug-Resistant Cancer, Study Shows

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Deepak Vaidya, chaiman

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