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ORGANIC SPECTROSCOPY

Read all about Organic Spectroscopy on ORGANIC SPECTROSCOPY INTERNATIONAL 

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DR ANTHONY MELVIN CRASTO Ph.D

DR ANTHONY MELVIN CRASTO Ph.D

DR ANTHONY MELVIN CRASTO, Born in Mumbai in 1964 and graduated from Mumbai University, Completed his Ph.D from ICT, 1991,Matunga, Mumbai, India, in Organic Chemistry, The thesis topic was Synthesis of Novel Pyrethroid Analogues, Currently he is working with AFRICURE PHARMA, ROW2TECH, NIPER-G, Department of Pharmaceuticals, Ministry of Chemicals and Fertilizers, Govt. of India as ADVISOR, earlier assignment was with GLENMARK LIFE SCIENCES LTD, as CONSUlTANT, Retired from GLENMARK in Jan2022 Research Centre as Principal Scientist, Process Research (bulk actives) at Mahape, Navi Mumbai, India. Total Industry exp 32 plus yrs, Prior to joining Glenmark, he has worked with major multinationals like Hoechst Marion Roussel, now Sanofi, Searle India Ltd, now RPG lifesciences, etc. He has worked with notable scientists like Dr K Nagarajan, Dr Ralph Stapel, Prof S Seshadri, etc, He did custom synthesis for major multinationals in his career like BASF, Novartis, Sanofi, etc., He has worked in Discovery, Natural products, Bulk drugs, Generics, Intermediates, Fine chemicals, Neutraceuticals, GMP, Scaleups, etc, he is now helping millions, has 9 million plus hits on Google on all Organic chemistry websites. His friends call him Open superstar worlddrugtracker. His New Drug Approvals, Green Chemistry International, All about drugs, Eurekamoments, Organic spectroscopy international, etc in organic chemistry are some most read blogs He has hands on experience in initiation and developing novel routes for drug molecules and implementation them on commercial scale over a 32 PLUS year tenure till date Feb 2023, Around 35 plus products in his career. He has good knowledge of IPM, GMP, Regulatory aspects, he has several International patents published worldwide . He has good proficiency in Technology transfer, Spectroscopy, Stereochemistry, Synthesis, Polymorphism etc., He suffered a paralytic stroke/ Acute Transverse mylitis in Dec 2007 and is 90 %Paralysed, He is bound to a wheelchair, this seems to have injected feul in him to help chemists all around the world, he is more active than before and is pushing boundaries, He has 100 million plus hits on Google, 2.5 lakh plus connections on all networking sites, 100 Lakh plus views on dozen plus blogs, 227 countries, 7 continents, He makes himself available to all, contact him on +91 9323115463, email amcrasto@gmail.com, Twitter, @amcrasto , He lives and will die for his family, 90% paralysis cannot kill his soul., Notably he has 38 lakh plus views on New Drug Approvals Blog in 227 countries......https://newdrugapprovals.wordpress.com/ , He appreciates the help he gets from one and all, Friends, Family, Glenmark, Readers, Wellwishers, Doctors, Drug authorities, His Contacts, Physiotherapist, etc He has total of 32 International and Indian awards

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Mangafodipir

August 4, 2014 11:50 am / 1 Comment on Mangafodipir


Mangafodipir

Mangafodipir.png

 

 Mangafodipir
CAS : 118248-94-5 (free acid); 155319-91-8 (hexahydrogen)
CAS Name: (OC-6-13)-[[N,N¢–1,2-Ethanediylbis[N-[[3-(hydroxy-kO)-2-methyl-5-[(phosphonooxy)methyl]-4-pyridinyl]methyl]glycinato-kN,kO]](8-)]manganate(6-)
Add Names: manganese(II)-N,N¢-dipyridoxylethylenediamine-N,N¢-diacetate-5,5-bis(phosphonate); manganese dipyridoxal diphosphate; MnDPDP
Manufacturers’ Codes: S-095
 C22H24MnN4O14P2
 685.33
Percent Composition: C 38.56%, H 3.53%, Mn 8.02%, N 8.18%, O 32.68%, P 9.04%
Mangafodipir 3D sticks.png
Clinical data
AHFS/Drugs.com Micromedex Detailed Consumer Information
Pregnancy cat. Not to be used
Routes Intravenous infusion
Pharmacokinetic data
Bioavailability NA
Protein binding 27% (manganese)
Negligible (DPDP)
Half-life 20 minutes (manganese)
50 minutes (DPDP)
Excretion Renal and fecal (manganese)
Renal (DPDP)
Identifiers
ATC code V08CA05
PubChem CID 3086672
ChemSpider 2343239 Yes
UNII N02W67RKJS Yes
Chemical data
Formula C22H28MnN4O14P2 
Mol. mass 689.362 g/mol
Diagnostic Aid (MRI Contrast Agent)
Manganese dipyridoxal diphosphate trisodium salt, Mangafodipir trisodium, Win-59010-2, S-095, MnDPDP, Teslascan

Mangafodipir (sold under the brand name Teslascan as mangafodipir trisodium) is a contrast agent delivered intravenously to enhance contrast in magnetic resonance imaging (MRI) of the liver. It has two parts, paramagnetic manganese (II) ions and thechelating agent fodipir (dipyridoxyl diphosphate, DPDP). Normal liver tissue absorbs the manganese more than abnormal or cancerous tissue. The manganese shortens the longitudinal relaxation time (T1), making the normal tissue appear brighter in MRIs. This enhanced contrast allows lesions to be more easily identified.

 

The condensation of pyridoxal 5-phosphate (I) with ethylenediamine (II) in methanol by means of NaOH gives the corresponding diimine (III), which is reduced with hydrogen over Pt/C in methanol/water yielding the expected diamine (IV). The reaction of (IV) with bromoacetic acid (V) by means of NaOH in methanol/water affords the N,N’-diacetic acid derivative (VI), which is finally treated with MnCl2 in water containing NaOH.

References

Literature References:
Paramagnetic manganese (II) chelate designed as a tissue specific imaging agent taken up by normal liver parenchyma. Prepn: S. M. Rocklage, S. C. Quay, EP 290047; eidem, US 4933456 (1988, 1990 both to Salutar); idem et al.,Inorg. Chem. 28, 477 (1989).
Pharmacology, toxicity and image enhancement studies: G. Elizondo et al., Radiology 178, 73 (1991).
HPLC determn in plasma: K. G. Toft et al., J. Pharm. Biomed. Anal. 15, 973 (1997).
Series of articles on clinical studies, toxicology and physicochemical properties: Acta Radiol. 38, 626-789 (1997).
Review of use as contrast agent for liver lesion detection: N. M. Rofsky, J. P. Earls, MRI Clin. North Am. 4, 73-85 (1996).
Properties: LD50 i.v. in mice: 5.4 mmol/kg (Elizondo).
Toxicity data: LD50 i.v. in mice: 5.4 mmol/kg (Elizondo)
……………………………………
Mangafodipir Trisodium
Click to View Image

C22H27MnN4Na3O14P2 757.33
Trisodium trihydrogen (OC-6-13)-[[N,N¢-1,2-ethanediylbis[N-[[3-hydroxy-2-methyl-5-[(phosphonooxy)methyl]-4-pyridinyl]methyl]glycinato]](8-)] manganate(6-).
Trisodium trihydrogen (OC-6-13)-[[N,N¢-ethylenebis[N-[[3-hydroxy-5-(hydroxymethyl)-2-methyl-4-pyridyl]methyl]glycine] 5,5¢-bis(phosphato)](8-)]manganate(6-) [140678-14-4].

Derivative Type: Trisodium salt
CAS Registry Number: 140678-14-4
Additional Names: Magnafodipir trisodium
Manufacturers’ Codes: Win-59010
Trademarks: Teslascan (Nycomed)
Molecular Formula: C22H27MnN4Na3O14P2
Molecular Weight: 757.32
Percent Composition: C 34.89%, H 3.59%, Mn 7.25%, N 7.40%, Na 9.11%, O 29.58%, P 8.18%
Properties: Pale yellow, triclinic hygroscopic crystals. d 1.537. uv max (water): 220, 257, 319 nm (e 37600, 10300, 13400). Soly (g/ml): 0.4596 water, 0.0230 methanol, 0.0008 ethanol, 0.0006 acetone, 0.0011 chloroform. Log P (1-octanol:water) -5.62; (1-butanol: water) -3.68. Prepd as 0.01 mmol/ml aqueous infusion: bright yellow, clear soln, pH 7.5. Viscosity (mPa.s): 1.0 at 20°, 0.7 at 37°. Osmolality (37°): 290 mosmol/kg. d20 1.01 g/ml.
Log P: Log P (1-octanol:water) -5.62; (1-butanol: water) -3.68
Absorption maximum: uv max (water): 220, 257, 319 nm (e 37600, 10300, 13400)
Density: d 1.537; d20 1.01 g/ml
Therap-Cat: Diagnostic aid (MRI contrast agent).

FDA Approves Dotarem, a New Magnetic Resonance Imaging Agent

March 21, 2013 9:37 am / 1 Comment on FDA Approves Dotarem, a New Magnetic Resonance Imaging Agent


Gadoterate meglumine     STR-  CREDIT PUBCHEM
Also known as: Magnescope, Magnescope (TN), AC1OCEY3, Meglumine gadoterate (JAN), EK-5504, D03355
Molecular Formula: C23H42GdN5O13
Molecular Weight: 753.85528
Cas No. 98059-18-8
 Name 2-[4,7-bis(carboxylatomethyl)-10-(carboxymethyl)-1,4,7, 10-tetrazacyclododec-1-yl]acetate; gadolinium(3+); (2R,3R,4R,5S)-6-(methylamino)hexane-1,2,3,4,5-pentol
MORE ABOUT STRUCTURE , CODE  CAS NO, ETC-  http://www.ama-assn.org/resources/doc/usan/gadoterate-meglumine.pdf
FDA Approves Dotarem, a New Magnetic Resonance Imaging Agent

March 20, 2013 — The U.S. Food and Drug Administration today approved Dotarem (gadoterate meglumine) for use in magnetic resonance imaging (MRI) of the brain, spine and associated tissues of patients ages 2 years and older.

Dotarem is a gadolinium-based contrast agent (GBCA) that helps radiologists see abnormalities on images of the central nervous system (CNS), the part of the body that contains the brain and spine, and surrounding tissues.

“Dotarem was shown to be a safe and effective magnetic resonance imaging agent in patients ages 2 years and older,” said Dwaine Rieves, M.D., director of the Division of Medical Imaging Products in the FDA’s Center for Drug Evaluation and Research. “Today’s approval provides doctors with another option to help evaluate anatomic abnormalities within the central nervous system.”

Dotarem (gadoterate meglumine)

Company: Guerbet
Treatment for: Diagnostic

Dotarem (gadoterate meglumine) is a gadolinium-based contrast agent under review for use in magnetic resonance imaging (MRI).

Dotarem is the only macrocyclic and ionic gadolinium-based contrast agent (GBCA) for the intravenous use with magnetic resonance imaging (MRI) in the brain (intracranial), spine and associated tissues in adults and pediatric patients to detect and visualize areas with disruption of the blood-brain barrier (BBB) and/or abnormal vascularity. The Guerbet NDA recommended dose is 0.1 mmol Gd/kg.

File:Gadoteric acid.png

Gadoteric acid

Gadoteric acid (trade names Artirem, Dotarem) is a macrocycle-structured gadolinium-based MRI contrast agent. It consists of the organic acid DOTA as a chelating agent, and gadolinium (Gd3+), and is used in form of the meglumine salt.[1] The drug is approved and used in a number of countries worldwide.[2]

  1. Herborn, C. U.; Honold, E.; Wolf, M.; Kemper, J.; Kinner, S.; Adam, G.; Barkhausen, J. (2007). “Clinical Safety and Diagnostic Value of the Gadolinium Chelate Gadoterate Meglumine (Gd-DOTA)”. Investigative Radiology 42 (1): 58–62. doi:10.1097/01.rli.0000248893.01067.e5. PMID 17213750. edit
  2. Drugs.com: Gadoteric Acid

A gadolinium chelate paramagnetic contrast agent. When placed in a magnetic field, gadoterate meglumine produces a large magnetic moment and so a large local magnetic field, which can enhance the relaxation rate of nearby protons; as a result, the signal intensity of tissue images observed with magnetic resonance imaging (MRI) may be enhanced. Because this agent is preferentially taken up by normal functioning hepatocytes, normal hepatic tissue is enhanced with MRI while tumor tissue is unenhanced. In addition, because gadobenate dimeglumine is excreted in the bile, it may be used to visualize the biliary system using MRI.

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