- PROCESS FOR MAKING CGRP RECEPTOR ANTAGONIST
-
The invention encompasses a novel process for making 2-[(8R)-8-(3,5-Difluorophenyl)-10-oxo-6,9-diazaspiro[4.5]dec-9-yl]-N-[(2R)-2'-oxo-1,1',2',3-tetrahydrospiro[indene-2,3'-pyrrolo[2,3-b]pyridin]-5-yl]acetamide, which is a CGRP receptor antagonist useful for the treatment of migraine, using an asymmetric phase-transfer catalysis route. The invention also encompasses an efficient and practical synthesis of the (R)-acid intermediate, and generates the benzylic stereocenter in an enantioselective manner.
- -
-
-
- Discovery of MK-3207: A highly potent, orally bioavailable CGRP receptor antagonist
-
Incorporation of polar functionality into a series of highly potent calcitonin gene-related peptide (CGRP) receptor antagonists was explored in an effort to improve pharmacokinetics. This strategy identified piperazinone analogues that possessed improved
- Bell, Ian M.,Gallicchio, Steven N.,Wood, Michael R.,Quigley, Amy G.,Stump, Craig A.,Zartman, C. Blair,Fay, John F.,Li, Chi-Chung,Lynch, Joseph J.,Moore, Eric L.,Mosser, Scott D.,Prueksaritanont, Thomayant,Regan, Christopher P.,Roller, Shane,Salvatore, Christopher A.,Kane, Stefanie A.,Vacca, Joseph P.,Selnick, Harold G.
-
scheme or table
p. 24 - 29
(2010/11/04)
-
