DRUG APPROVALS BY DR ANTHONY MELVIN CRASTO
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The α-tocopherol form of vitamin E
Vitamin E refers to a group of eight fat-soluble compounds that include both tocopherolsand tocotrienols.[1] There are many different forms of vitamin E, of which γ-tocopherol is the most common in the North American diet.[2] γ-Tocopherol can be found in corn oil, soybean oil, margarine and dressings.[3][4] In the North American diet, α-Tocopherol, the most biologically active form of vitamin E, is the second most common form of vitamin E. This variant of vitamin E can be found most abundantly in wheat germ oil, sunflower, and safflower oils.[4][5] It is a fat-soluble antioxidant that stops the production of reactive oxygen species formed when fat undergoes oxidation.[6][7][8]
- Synthesis of Vitamin E
Vitamin E (CAS NO.: 59-02-9), with other names as 2(R),5,7,8-Tetramethyl-2-[4(R),8(R),12-trimethyltridecyl]-3,4-dihydro-2H-1-benzopyran-6-ol, could be produced through the following synthetic routes.
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References
- Brigelius-Flohe, B; Traber (1999). “Vitamin E: function and metabolism”. FASEB 13: 1145–1155.
- Traber, MG (1998). “The biological activity of vitamin E”. The Linus Pauling Institute. Retrieved 6 March 2011.
- Bieri, JG; Evarts (1974). “γ-Tocopherol: metabolism, biological activity and significance in human vitamin E nutrition”. American Journal of Clinical Nutrition 27 (9): 980–986. PMID 4472121.
- Brigelius-Flohé R, Traber MG (1 July 1999). “Vitamin E: function and metabolism”. FASEB J. 13 (10): 1145–55. PMID 10385606.
- Reboul E, Richelle M, Perrot E, Desmoulins-Malezet C, Pirisi V, Borel P (15 November 2006). “Bioaccessibility of carotenoids and vitamin E from their main dietary sources”. Journal of Agricultural and Food Chemistry 54 (23): 8749–8755. doi:10.1021/jf061818s.PMID 17090117.
- National Institute of Health (4 May 2009). “Vitamin E fact sheet”.
- Herrera; Barbas, C (2001). “Vitamin E: action, metabolism and perspectives”. Journal of Physiology and Biochemistry 57 (2): 43–56.doi:10.1007/BF03179812. PMID 11579997.
- Packer L, Weber SU, Rimbach G (2001). “Molecular aspects of α-tocotrienol antioxidant action and cell signalling”. Journal of Nutrition 131 (2): 369S–73S. PMID 11160563.
- Vitamin E bound to proteins in the PDB
- Vitamin E Medline Plus, Medical Encyclopedia, U.S. National Library of Medicine
- Vitamin E Office of Dietary Supplements, National Institutes of Health
- Jane Higdon, “Vitamin E“, Micronutrient Information Center, Linus Pauling Institute, Oregon State University
- Vitamin E Food Charts
DR ANTHONY MELVIN CRASTO Ph.D
DR ANTHONY CRASTO, PhD, ICT Organic chemistry, Currently working with GLENMARK GENERICS LTD research centre as Principal Scientist, process research (bulk actives) at Mahape, Navi Mumbai, India, helping millions, million hits on google on all organic chemistry websites, Hands on experience in developing novel routes for drug molecules and implementation on commercial scale. several international patents published.pushing boundaries, one lakh connections on all networking sites
Donepezil, marketed under the trade name Aricept by its developer Eisai and partner Pfizer, is a centrally acting reversible acetylcholinesterase inhibitor.[1]Its main therapeutic use is in the palliative treatment of mild to moderateAlzheimer’s disease.[2] Common side effects include gastrointestinal upset. It has an oral bioavailability of 100% and easily crosses the blood–brain barrier. Because it has a half-life of about 70 hours, it can be taken once a day.
(RS)-2-[(1-benzyl-4-piperidyl)methyl]- 5,6-dimethoxy-2,3-dihydroinden-1-one
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Synthesis
The condensation of 5,6-dimethoxy-1-indanone (I) with 1-benzylpiperidine-4-carboxaldehyde (II) by means of butyl lithium 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 (1,2).
Manufacturer Eisai Co., Ltd. (Japan).
References
1. Sugimoto, H., Tsuchiya, Y., Higurashi, K. et al. (Eisai Co., Ltd.) Cyclic amine cpd., its use and pharmaceutical compsns. comprising it. AU 8818216, EP 296560, JP 89079151, US 4895841.
2. Iimura, Y., Mishima, M., Sugimoto, H. Synthesis of 1-benzyl-4-[(5,6-dimethoxy[2-14C]-1-indanon)-2-yl]methylpiperidine hydrochloride (E-2020-14C). J Label Compound Radiopharm 1989, 27(7): 835-9.
- 1 Birks J, Harvey RJ (2006). Birks, Jacqueline. ed. “Donepezil for dementia due to Alzheimer’s disease”. Cochrane Database Syst Rev (1): CD001190.doi:10.1002/14651858.CD001190.pub2. PMID 16437430.
- 2 “aricept”. The American Society of Health-System Pharmacists. Retrieved 3 April 2011.
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SPECTROSCOPY
MASS
13C NMR
DEPT 90 C13 NMR
DEPT135
IR
1H NMR
COSY 1H NMR
HSQC NMR
HMBC NMR
DR ANTHONY MELVIN CRASTO Ph.D ( ICT, Mumbai) , INDIA 25Yrs Exp. in the feld of Organic Chemistry,Working for GLENMARK GENERICS at Navi Mumbai, INDIA. Serving chemists around the world. Helping them with websites on Chemistry.Million hits on google NO ADVERTISEMENTS , ACADEMIC , NON COMMERCIAL SITE, world acclamation from industry, academia, drug authorities for websites, blogs and educational contribution,email or call now for sure success formula, amcrasto@gmail.com, 9323115463. you can swim to the shore even if you are drowned in a storm.
Sertraline hydrochloride (trade names Zoloft and Lustral, among others) is anantidepressant of the selective serotonin reuptake inhibitor (SSRI) class. It was discovered byPfizer. Sertraline is primarily used to treat major depression in adult outpatients as well asobsessive–compulsive, panic, and social anxiety disorders in both adults and children
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Schematic Representation for Synthesis of Sertraline
Conditions:-
i. Benzene, anhydrous aluminum chloride, dichloromethane,
ii. Diethyl succinate, potassium-t-butoxide, t-butyl alcohol, reflux, 16 h,
iii. 48% aqueous HBr, acetic acid, reflux, 36 h,
iv. Hydrogen gas (1 atm), 5% Pd/c catalyst, ethyl acetate, room temperature, 24 h,
v. a) Thionyl chloride, toluene, reflux, 75 min b) anhydrous aluminum chloride, carbon disulfide, room temperature, 16 h,
vi. Methylamine, tetrahydrofuran, titanium tetrachloride, room temperature, 17 h,
vii. a) Hydrogen gas (1 atm), 10% Pd/c catalyst, tetrahydrofuran, room temperature, 2 h b) Gaseous hydrogen chloride,
viii. Crystallization from methanol and ether,
ix) a) 20% sodium hydroxide, ethyl acetate b) D (-) Mandelic acid, ethanol, resolution
Sertraline
CAS No:- [79617-96-2]
IUPAC Name:- (1S,4S)-4-(3,4-Dichlorophenyl)-1,2,3,4-tetrahydro-N-methyl-1-naphthalenamine
MW: 306.23
Drug information:- Sertraline is an anti-depressant drug.
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DR ANTHONY MELVIN CRASTO Ph.D ( ICT, Mumbai) , INDIA 25Yrs Exp. in the feld of Organic Chemistry,Working for GLENMARK GENERICS at Navi Mumbai, INDIA. Serving chemists around the world. Helping them with websites on Chemistry.Million hits on google NO ADVERTISEMENTS , ACADEMIC , NON COMMERCIAL SITE, world acclamation from industry, academia, drug authorities for websites, blogs and educational contribution,email or call now for sure success formula, amcrasto@gmail.com, 9323115463. you can swim to the shore even if you are drowned in a storm.
2-acetoxybenzoic acid
Aspirin (USAN), also known as acetylsalicylic acid is a salicylate drug, often used as an analgesic to relieve minor aches and pains, as an antipyretic to reduce fever, and as an anti-inflammatorymedication. Aspirin was first isolated by Felix Hoffmann, a chemist with the German company Bayer in 1897.[1][2]
Salicylic acid, the main metabolite of aspirin, is an integral part of human and animal metabolism. While in humans much of it is attributable to diet, a substantial part is synthesized endogenously.[3]
Aspirin also has an antiplatelet effect by inhibiting the production of thromboxane, which under normal circumstances binds platelet molecules together to create a patch over damaged walls of blood vessels. Because the platelet patch can become too large and also block blood flow, locally and downstream, aspirin is also used long-term, at low doses, to help prevent heart attacks, strokes, and blood clot formation in people at high risk of developing blood clots.[4] It has also been established that low doses of aspirin may be given immediately after a heart attack to reduce the risk of another heart attack or of the death of cardiac tissue.[5][6] Aspirin may be effective at preventing certain types of cancer, particularly colorectal cancer.[7][7][8][9]
The main undesirable side effects of aspirin taken by mouth are gastrointestinal ulcers, stomach bleeding, and tinnitus, especially in higher doses. In children and adolescents, aspirin is no longer indicated to control flu-like symptoms or the symptoms of chickenpoxor other viral illnesses, because of the risk of Reye’s syndrome.[10]
Advertisement for Aspirin,
Aspirin is part of a group of medications called nonsteroidal anti-inflammatory drugs(NSAIDs), but differs from most other NSAIDs in the mechanism of action. Though it, and others in its group called the salicylates, have similar effects (antipyretic, anti-inflammatory, analgesic) to the other NSAIDs and inhibit the same enzymecyclooxygenase, aspirin (but not the other salicylates) does so in an irreversible manner and, unlike others, affects more the COX-1 variant than the COX-2 variant of the enzyme.[11]
Today, aspirin is one of the most widely used medications in the world, with an estimated 40,000 tonnes of it being consumed each year.[12] In countries where Aspirin is a registered trademark owned by Bayer, the generic term is acetylsalicylic acid (ASA).[13]
1923 advertisement
Synthesis
The synthesis of aspirin is classified as an esterification reaction. Salicylic acid is treated with acetic anhydride, an acid derivative, causing a chemical reaction that turns salicylic acid’s hydroxyl group into an ester group (R-OH → R-OCOCH3). This process yields aspirin and acetic acid, which is considered a byproduct of this reaction. Small amounts of sulfuric acid (and occasionally phosphoric acid) are almost always used as a catalyst. This method is commonly employed in undergraduate teaching labs.[104]
- Reaction Mechanism
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- Sneader, W. (2000). “The discovery of aspirin: A reappraisal”. BMJ (Clinical research ed.) 321 (7276): 1591–1594. doi:10.1136/bmj.321.7276.1591. PMC 1119266.PMID 11124191. edit
- Karsten Schrör (2009). Acetylsalicylic acid. ISBN 978-3-527-32109-4.
- Paterson, John R.; Baxter, Gwendoline; Dreyer, Jacob S.; Halket, John M.; Flynn, Robert; Lawrence, James R. (2008).“Salicylic Acid sans Aspirin in Animals and Man: Persistence in Fasting and Biosynthesis from Benzoic Acid”. Journal of Agricultural and Food Chemistry 56 (24): 11648–11652.doi:10.1021/jf800974z. PMC 2800778.PMID 19053387. edit
- Lewis, H D; J W Davis, D G Archibald, W E Steinke, T C Smitherman, J E Doherty, H W Schnaper, M M LeWinter, E Linares, J M Pouget, S C Sabharwal, E Chesler, H DeMots (18 August 1983). “Protective effects of aspirin against acute myocardial infarction and death in men with unstable angina. Results of a Veterans Administration Cooperative Study”. The New England Journal of Medicine 309 (7): 396–403.doi:10.1056/NEJM198308183090703. ISSN 00284793.PMID 6135989.
- Julian, D G; D A Chamberlain, S J Pocock (24 September 1996). “A comparison of aspirin and anticoagulation following thrombolysis for myocardial infarction (the AFTER study): a multicentre unblinded randomised clinical trial”. BMJ (British Medical Journal) 313 (7070): 1429–1431.doi:10.1136/bmj.313.7070.1429. PMC 2353012.PMID 8973228.
- Krumholz, Harlan M.; Martha J. Radford, Edward F. Ellerbeck, John Hennen, Thomas P. Meehan, Marcia Petrillo, Yun Wang, Timothy F. Kresowik, Stephen F. Jencks (1995). “Aspirin in the Treatment of Acute Myocardial Infarction in Elderly Medicare Beneficiaries : Patterns of Use and Outcomes”. Circulation 92(10): 2841–2847. PMID 7586250.
- Algra, Annemijn M; Rothwell, Peter M (2012). “Effects of regular aspirin on long-term cancer incidence and metastasis: A systematic comparison of evidence from observational studies versus randomised trials”. The Lancet Oncology.doi:10.1016/S1470-2045(12)70112-2.
- Rothwell, Peter M; Price, Jacqueline F; Fowkes, F Gerald R; Zanchetti, Alberto; Roncaglioni, Maria Carla; Tognoni, Gianni; Lee, Robert; Belch, Jill FF et al. (2012). “Short-term effects of daily aspirin on cancer incidence, mortality, and non-vascular death: Analysis of the time course of risks and benefits in 51 randomised controlled trials”. The Lancet. doi:10.1016/S0140-6736(11)61720-0. Rothwell, Peter M; Wilson, Michelle; Price, Jacqueline F; Belch, Jill FF; Meade, Tom W; Mehta, Ziyah (2012). “Effect of daily aspirin on risk of cancer metastasis: A study of incident cancers during randomised controlled trials”. The Lancet.doi:10.1016/S0140-6736(12)60209-8.
- Macdonald S (2002). “Aspirin use to be banned in under 16 year olds”. BMJ 325 (7371): 988.doi:10.1136/bmj.325.7371.988/c. PMC 1169585.PMID 12411346.
- Burke, Anne; Smyth, Emer; FitzGerald, Garret A. (2006). “26: Analgesic Antipyretic and Antiinflammatory Agents”.Goodman and Gilman’s the pharmacological basis of therapeutics (11 ed.). New York: McGraw-Hill. pp. 671–716.ISBN 978-0-07-142280-2.
- Warner, T. D.; Warner TD, Mitchell JA (2002).“Cyclooxygenase-3 (COX-3): filling in the gaps toward a COX continuum?”. Proc Natl Acad Sci USA 99 (21): 13371–3.doi:10.1073/pnas.222543099. PMC 129677.PMID 12374850.
- “The use of aspirin”. Wordconstructions.com. Retrieved 11 May 2011.
- DR ANTHONY MELVIN CRASTO Ph.Damcrasto@gmail.com
MOBILE-+91 9323115463GLENMARK SCIENTIST , NAVIMUMBAI, INDIA
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DR ANTHONY MELVIN CRASTO Ph.D , Born in Mumbai in 1964 and graduated from Mumbai University, Completed his PhD from ICT ,1991, Mumbai, India in Organic chemistry, The thesis topic was Synthesis of Novel Pyrethroid Analogues,
Currently he is working with GLENMARK- GENERICS LTD, Research centre as Principal Scientist, Process Research (bulk actives) at Mahape, Navi Mumbai, India.
Prior to joining Glenmark, he worked with major multinationals like Hoechst Marion Roussel, now Sanofi Aventis, & Searle India ltd, now Rpg lifesciences, etc. He has worked in Basic research, Neutraceuticals, Natural products, Flavors, Fragrances, Pheromones, Vet Drugs, Drugs, formulation, GMP etc. He has total 25 yrs exp in this field, he is now helping millions, has million hits on google on all organic chemistry websites.
His New Drug Approvals , Green Chemistry International, Eurekamoments in Organic Chemistry , Organic Chemistry by Dr Anthony, WIX BLOG , are some most read chemistry blogs
He has hands on experience in initiation and developing novel routes for drug molecules and implementation them on commercial scale over a 25 year tenure, good knowledge of IPM, GMP, Regulatory aspects, he has several international drug patents published worldwide .
He has good proficiency in Technology Transfer, Spectroscopy , Stereochemistry , Synthesis, Reactions in Org Chem , Polymorphism, Pharmaceuticals , Medicinal chemistry , Organic chemistry literature , Patent related site , Green chemistry , Reagents , R & D , Molecules , Heterocyclic chem , Sourcing etc
He suffered a paralytic stroke in dec 2006 and is bound to a wheelchair, this seems to have injected feul in him to help chemists around the world, he is more active than before and is pushing boundaries, he has one lakh connections on all networking sites, He makes himself available to all, contact him on +91 9323115463, amcrasto@gmail.com
New Drug Approvals 
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P.S My apologies for getting off-topic but I had to ask!