1409944-01-9

Upstream product

• 1409944-26-8 tert-butyl (4R,7S,8S)-7-(2,3-difluorophenyl)-4-hydroxy-5,6,7,8-tetrahydro-4H-cyclohepta[d]thiazol-8-ylcarbamate 
• 112587-04-9 (E)-1-nitrohexa-1,5-diene 
• 1409944-27-9 (4R,7S,8S)-8-(tert-butoxycarbonylamino)-7-(2,3-difluorophenyl)-5,6,7,8-tetrahydro-4H-cyclohepta[d]thiazol-4-yl 4-(2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxylate 
• 1409944-25-7 tert-butyl (7S,8S)-7-(2,3-difluorophenyl)-4-oxo-5,6,7,8-tetrahydro-4H-cyclohepta[d]thiazol-8-ylcarbamate 
• 1409944-23-5 (E)-methyl 2-((7S,8S)-8-(tert-butoxycarbonylamino)-7-(2,3-difluorophenyl)-5,6,7,8-tetrahydro-4H-cyclohepta[d]thiazol-4-ylidene)acetate 
• 1409944-21-3 (6S,7S,E)-methyl 7-(4-bromothiazol-5-yl)-7-(tert-butoxycarbonylamino)-6-(2,3-difluorophenyl)hept-2-enoate 
• 1409944-19-9 tert-butyl (1S,2S)-1-(4-bromothiazol-5-yl)-2-(2,3-difluorophenyl)hex-5-enylcarbamate 
• 1409944-17-7 (1S,2S)-1-(4-bromothiazol-5-yl)-2-(2,3-difluorophenyl)hex-5-en-1-amine 
• 1409944-06-4 (R)-N-((1S,2S)-1-(3-bromopyrazin-2-yl)-2-(2,3-difluorophenyl)hex-5-enyl)-2-methylpropane-2-sulfinamide 
• 1409944-05-3 (R,E)-N-((S)-2-(2,3-difluorophenyl)hex-5-enylidene)-2-methylpropane-2-sulfinamide 
• 1409944-04-2 (S)-2-(2, 3-difluorophenyl)hex-5-enal 
• 1409944-03-1 (S)-1,2-difluoro-3-(1-nitrohex-5-en-2-yl)benzene 

Relevant academic research and scientific papers

Asymmetric Synthesis of Heterocyclic Analogues of a CGRP Receptor Antagonist for Treating Migraine

An asymmetric synthesis of novel heterocyclic analogue of the CGRP receptor antagonist rimegepant (BMS-927711, 3) is reported. The cycloheptane ring was constructed by an intramolecular Heck reaction. The application of Hayashi-Miyaura and Ellman reactions furnished the aryl and the amine chiral centers, while the separable diastereomeric third chiral center alcohols led to both carbamate and urea analogues. This synthetic approach was applicable to both 6- and 5-membered heterocycles as exemplified by pyrazine and thiazole derivatives.

CGRP RECEPTOR ANTAGONISTS

The disclosure generally relates to the novel compounds of formula (I), including pharmaceutically acceptable salts, which are CGRP receptor antagonists. The disclosure also relates to pharmaceutical compositions and methods for using the compounds in the treatment of CGRP related disorders including migraine and other headaches, neurogenic vasodilation, neurogenic inflammation, thermal injury, circulatory shock, flushing associated with menopause, airway inflammatory diseases such as asthma, and chronic obstructive pulmonary disease (COPD).