Institutionen för kliniska vetenskaper, Lund - Forskningsoutput

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. CGRP and its receptors are found in areas of the central and peripheral nervous system that are important for the transmission of 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. 67 A first generation route to the API suitable for pilot plant manufacturing had previously been developed (Scheme 12).

128 Development was terminated when elevated levels of the liver enzyme alanine transaminase were found in treated patients. Thieme E-Books & E-Journals. Full-text search Full-text search; Author Search; Title Search; DOI Search SoS C-1 Building Blocks in Organic Synthesis SoS Multicomponent Reactions SoS Cross Coupling and Heck-Type Reactions Weitere E-Angebote Science of Synthesis Pharmaceutical Substances The difference in pain relief at 2 hours significantly favored telcagepant over placebo (odds ratio = 2.48, 95% confidence interval = 2.18-2.81, P < 0.001). The difference in pain relief at 2 hours did not significantly favor telcagepant over triptans or vice versa (OR = 0.76, 95 % CI: 0.57 to 1.01, p = 0.061).

André Erdling - Research Outputs - Lund University

On His Wings Travels knows how. 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.

André Erdling - Research Outputs - Lund University

Telcagepant (code name MK-0974) is a calcitonin gene-related peptide receptor antagonist which was an investigational drug for the acute treatment and prevention of migraine, developed by Merck & Co. In the acute treatment of migraine, it was found to have equal potency to rizatriptan [1] and zolmitriptan [2] in two Phase III clinical trials . 2017-01-25 · Here Xu et al. 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.

Welcome to PubChem! SYNTHESIS OF TELCAGEPANT Stanislav Rádl .
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A highly efficient, asymmetric synthesis of telcagepant (1), a CGRP receptor antagonist for the treatment of migraine, is described. This synthesis features the first application of iminium 2008-07-01 · The latter route has been implemented to produce multigram quantities of telcagepant for extensive preclinical evaluation. Synthesis of the (3R,6S)-3-Amino-6-(2,3-difluorophenyl)azepan-2-one of Telcagepant (MK-0974), a Calcitonin Gene-Related Peptide Receptor Antagonist for the Treatment of Migraine Headache | Organic Letters. Second part of the synthesis of Telcagepant.

Synthesis Reference. Leonardo R. Allain, et. al., "Formulations for CGRP receptor antagonists." Australian Patent AU2014318741B2, published December 06, 2018.
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Institutionen för kliniska vetenskaper, Lund - Forskningsoutput

Moreno-Ajona D, Chan C, Villar-Martinez MD, Goadsby PJ: Targeting CGRP and 5-HT1F Receptors for the Acute Therapy of Migraine: A Literature Review. Figure 9: The total synthesis of telcagepant by Merck.

André Erdling - Research Outputs - Lund University

Synthesis of the (3R,6S)-3-Amino-6-(2,3-difluorophenyl)azepan-2-one of Telcagepant (MK-0974), a Calcitonin Gene-Related Peptide Receptor Antagonist for the Treatment of Migraine Headache | Organic Letters.

Facebook. Second part of the synthesis of Telcagepant. Cyclisation involved the employment of a mixed anhydride, possible for the decreased nucleophilicity of the trifluoroethyl nitrogen, and was followed by a base promoted dynamic crystallisation process in aqueous NaOH/DMSO mixture, which allowed the isolation of the 2-acetamido caprolactam 60 in 73% overall yield from the enamide. Telcagepant, is not in stock, may be available through custom synthesis. For cost-effective reason, minimum 1 gram order is requested. The product will be characterized by NMR, HPLC and MS analysis.