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Jan Stach, Jan Doubský . The 24th International Society of . Heterocyclic Chemistry Congress. September 8-13, 2013. Shanghai .

Telcagepant synthesis

This synthesis features the first application of … Synthesis of Telcagepant Significance: Telcagepant is a selective antago-nist of calcitonin gene related peptide (CGRP) that is in phase clinical trials for the treatment of mi-graine. The synthesis featured an enantioselective 1,4-addition of nitromethane, which is the first application of … Asymmetric Synthesis of Telcagepant, a CGRP Receptor Antagonist for the Treatment of Migraine Feng Xu,* Michael Zacuto, Naoki Yoshikawa, Richard Desmond, Scott Hoerrner, Tetsuji Itoh, Michel Journet, Guy Humphrey, Cameron Cowden, Neil Strotman, Paul Devine Department of Process Research, Merck Research Laboratories, Rahway, NJ 07065, USA 2006-10-26. Telcagepant has been investigated for the treatment of Migraine. It is an antagonist of the receptor for calcitonin gene-related peptide (CGRP), a primary neuropeptide involved in the pathophysiology of migraine. CGRP and its receptors are found in areas of the central and peripheral nervous system that are important for the The first large-scale application of asymmetric iminium ion catalysis has been reported by Xu et al. at Merck as a key step in an improved process for synthesis of telcagepant (68, Scheme 12), a calcitonin gene-related peptide (CGRP) receptor antagonist indicated for the treatment of acute migraine.

Second part of the synthesis of Telcagepant. olcegepant (BIBN4096BS) and telcagepant (MK-0974), can treat migraine. Calcitonin gene-related peptide stimulation of nitric oxide synthesis and release 19 Mar 2018 CGRP belongs to the calcitonin family and is synthesized from either Telcagepant was the first oral CGRP receptor antagonists developed 12 Sep 2019 After synthesis, CGRP is transported by vesicles to the axon terminal.4 study of telcagepant in patients with stable angina pectoris.

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2010, 75, 7829−7841). The route described in the report is an example of a synthetic target driving the discovery of new chemistries.

André Erdling - Research Outputs - Lund University

It is an antagonist of the receptor for calcitonin gene-related peptide (CGRP), a primary neuropeptide involved in the pathophysiology of migraine.

Welcome to PubChem! SYNTHESIS OF TELCAGEPANT Stanislav Rádl . Jan Stach, Jan Doubský .
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Request a free consultation now Figure 9: The total synthesis of telcagepant by Merck. - "Domino and one-pot syntheses of biologically active compounds using diphenylprolinol silyl ether" Weitere E-Angebote Science of Synthesis Pharmaceutical Substances Two novel routes have been developed to the (3 R,6 S)-3-amino-6-(2,3-difluorophenyl)-1-(2,2,2-trifluoroethyl)azepan-2-one 2 of the CGRP receptor antagonist clinical candidate telcagepant (MK-0974, 1). The first employs a ring-closing metathesis of the styrene 7 as the key reaction, while the second makes use of a highly diastereoselective Hayashi-Miyaura Rh-catalyzed arylboronic acid addition Thieme E-Books & E-Journals. Full-text search Full-text search; Author Search; Title Search; DOI Search Thieme E-Books & E-Journals. Jahre (Archiv) 2010 Isolating only three intermediates, the overall yield of this cost-effective synthesis was up to 27%.

Calcitonin gene-related peptide stimulation of nitric oxide synthesis and release 19 Mar 2018 CGRP belongs to the calcitonin family and is synthesized from either Telcagepant was the first oral CGRP receptor antagonists developed 12 Sep 2019 After synthesis, CGRP is transported by vesicles to the axon terminal.4 study of telcagepant in patients with stable angina pectoris. The use. 18 Oct 2010 A highly efficient, asymmetric synthesis of telcagepant (1), a CGRP receptor antagonist for the treatment of migraine, is described.
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André Erdling - Research Outputs - Lund University

of Merck Rahway disclose their efforts towards an improved multikilogram synthesis of telcagepant, a CGRP receptor antagonist for the treatment of migraines ( J. Org. Chem. 2010, 75, 7829−7841). The route described in the report is an example of a synthetic target driving the discovery of new chemistries.

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André Erdling - Research Outputs - Lund University

Full-text search Full-text search; Author Search; Title Search; DOI Search MK-0974 (Telcagepant) is a potent and selective antagonist of the human and rhesus CGRP receptors.

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67 A first generation route to the API suitable for pilot plant manufacturing had previously been developed (Scheme 12).

The | Find, read and cite all the research you Disclosed is an efficient synthesis for the manufacture of the caprolactam intermediate (3R,6S)-3-amino-6-(2,3-difluorophenyl)-1-(2,2,2-trifluoroethyl) azepan-2-one: Formula and salts thereof, and an efficient preparation of telcagepant using the caprolactam intermediate. 2006-10-26. Telcagepant has been investigated for the treatment of Migraine. It is an antagonist of the receptor for calcitonin gene-related peptide (CGRP), a primary neuropeptide involved in the pathophysiology of migraine.