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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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Cenacitinib

January 15, 2026 2:47 am / Leave a comment


Cenacitinib

CAS 2641636-52-2

MF C19H19F2N7O3 MW431.4

Urea, N-[(1R,2S)-2-fluorocyclopropyl]-N′-[5-[(7-fluoro-2,3-dihydro-1,4-benzodioxin-5-yl)amino]-7-(methylamino)pyrazolo[1,5-a]pyrimidin-3-yl]-

N-{5-[(7-fluoro-2,3-dihydro-1,4-benzodioxin-5-yl)amino]-7-(methylamino)pyrazolo[1,5-a]pyrimidin-3-yl}-N′-[(1R,2S)-2-fluorocyclopropyl]urea

Janus kinase inhibitor, anti-inflammatory, VTX958, VTX 958, SB88R8KGL3

VTX958 for the Treatment of Moderately to Severely Active Crohn’s Disease

CTID: NCT05688852

Phase: Phase 2

Status: Terminated

Date: 2025-07-03

SYN

[US20210139486]

https://patentscope.wipo.int/search/en/detail.jsf?docId=US323750705&_cid=P22-MKEUDK-45432-1

Example 4: Synthesis of 1-(5-((7-fluoro-2,3-dihydrobenzo[b][1,4]dioxin-5-yl)amino)-7-(methylamino)pyrazolo[1,5-a]pyrimidin-3-yl)-3-((1R,2S)-2-fluorocyclopropyl)urea (5)

Step 1: To a solution of 1E (100 g, 288 mmol) and 2E (57 g, 345 mmol) in dry 1,4-dioxane (3000 mL) under N 2 atmosphere was added Cs 2CO 3 (141 g, 432 mmol), Pd(OAc) 2 (5.2 g, 23.3 mmol) and BINAP (28.6 g, 46.6 mmol). After stirring at 115° C. overnight, the reaction mixture was cooled to rt. and diluted with hexane (3000 mL). The solid was collected by filtration and washed with 2×1500 mL (50% hexane in DCM). The solid was suspended into 5000 mL water and stirred for 1 h. The solid was collected by filtration and dried under vacuum to afford compound 2 (90 g, 65%) as a brown solid.
      Step 2: To a solution of compound 2 (70 g, 145 mmol) in NMP (2000 mL) was added saturated NH 4Cl (aq., 1000 mL) and Fe (92.8 g, 1.45 mol). After stirring at 80° C. for 5.0 hours, the reaction mixture was cooled to rt. and filtrated. The filtrate was poured into water (20 L) and the solid was collected by filtration. The solid was dissolved with DCM (˜1500 mL) and flashed through a short silica gel column, the column was washed with another 3000 mL of DCM/MeOH=30/1. The organic phases were concentrated under vacuum. The residue was triturated by EtOH/MeCN (2000 mL, 5/1, v/v). The solid was collected by filtration and dried under vacuum to afford compound 3 (46 g, 71%) as a brown solid.
      Step 3: To a solution of compound 3 (86 g, 0.19 mol, 1.0 eq.) in DMF (800 mL) was added 3C (44.7 g, 0.23 mol, 1.3 eq.) and TEA (38.6 g, 0.38 mol, 2 eq.). After stirring at 80° C. for 2 hours, the reaction mixture was cooled to RT and poured into water (8000 mL). The solid was collected by filtration and dried under vacuum. The residue was triturated by EtOH/MeCN (1200 mL, 5/1, v/v). The solid was collected by filtration and dried under vacuum to afford compound 4 (75 g, 71%) as a brown solid.
      Step 4: To a solution of compound 4 (118 g, 0.21 mol, 1.0 eq.) in DCM (1200 mL) was added triethylsilane (37.3 g, 0.32 mol, 1.5 eq.). After stirring for 10 mins, TFA (240 mL) was added into the mixture and the reaction solution was stirred at rt. for 0.5 hour. TfOH (60 mL) was added and the reaction solution was stirred at rt. for another 2 hour. The reaction mixture was poured into saturated NaHCO 3 (30 mL). The solid was collected by filtration and dried under vacuum. The solid was triturated with EtOH (500 mL) and collected by filtration. The solid was triturated with EtOAc (2×500 mL). The solid was collected by filtration and dried under vacuum to afford 1-(5-((7-fluoro-2,3-dihydrobenzo[b][1,4]dioxin-5-yl)amino)-7-(methylamino)pyrazolo[1,5-a]pyrimidin-3-yl)-3-((1R,2S)-2-fluorocyclopropyl)urea (5) (80 g, 86%) as a yellow solid. LCMS: 432.1 [M+H] +.

PAT

Tyk2 pseudokinase ligands

Publication Number: US-2021139486-A1

Priority Date: 2019-11-08

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//////cenacitinib, cenacitinib, Janus kinase inhibitor, anti-inflammatory, VTX958, VTX 958, SB88R8KGL3

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ANAX LABORATORIES

WEBSITE https://www.anaxlab.com/

Discovery Solutions, Supporting the chemistry needs of clients in the Medical, Analytical and Bio Sciences

Development Solutions, Developing from Lab scale to PR&D, Kilo Scale-ups and Commercial Scales

SEE MORE………Integrated Solutions, Manufacturing Solutions, Products,
Can’t Find? Let’s Connect

Phone : +91 897704 2010 /  +91 9177075735, Email : info@anaxlab.com