An efficient, direct bis-ortho-chlorination of 4-(difluoromethoxy)aniline and its application to the synthesis of BMS-665053, a potent and selective pyrazinone-containing corticotropin-releasing factor-1 receptor antagonist
An efficient scale-up synthesis of (S)-5-chloro-1-(1-cyclopropylethyl)-3- (2,6-dichloro-4-(difluoromethoxy)phenylamino)-pyrazin-2(1H)-one, 1 (BMS-665053), is described. This new process features a one-step direct bis-ortho- chlorination of 4-(difluorometh
Li, Jianqing,Smith, Daniel,Krishnananthan, Subramaniam,Hartz, Richard A.,Dasgupta, Bireshwar,Ahuja, Vijay,Schmitz, William D.,Bronson, Joanne J.,Mathur, Arvind,Barrish, Joel C.,Chen, Bang-Chi
p. 156 - 159
(2012/05/20)
In vitro intrinsic clearance-based optimization of N3- phenylpyrazinones as corticotropin-releasing factor-1 (CRF1) receptor antagonists
A series of pyrazinone-based heterocycles was identified as potent and orally active corticotropinreleasing factor-1 (CRF1) receptor antagonists. Selected compounds proved efficacious in an anxiety model in rats; however, pharmacokinetic proper
Hartz, Richard A.,Ahuja, Vijay T.,Rafalski, Maria,Schmitz, William D.,Brenner, Allison B.,Denhart, Derek J.,Ditta, Jonathan L.,Deskus, Jeffrey A.,Yue, Eddy W.,Arvanitis, Argyrios G.,Lelas, Snjezana,Li, Yu-Wen,Molski, Thaddeus F.,Wong, Harvey,Grace, James E.,Lentz, Kimberley A.,Li, Jianqing,Lodge, Nicholas J.,Zaczek, Robert,Combs, Andrew P.,Olson, Richard E.,Mattson, Ronald J.,Bronson, Joanne J.,Macor, John E.
experimental part
p. 4161 - 4172
(2010/02/28)
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