Triphenylethanamine Derivatives as Cholesteryl Ester Transfer Protein Inhibitors: Discovery of N-[(1R)-1-(3-Cyclopropoxy-4-fluorophenyl)-1-[3-fluoro-5-(1,1,2,2-tetrafluoroethoxy)phenyl]-2-phenylethyl]-4-fluoro-3-(trifluoromethyl)benzamide (BMS-795311)
Cholesteryl ester transfer protein (CETP) inhibitors raise HDL-C in animals and humans and may be antiatherosclerotic by enhancing reverse cholesterol transport (RCT). In this article, we describe the lead optimization efforts resulting in the discovery o
Qiao, Jennifer X.,Wang, Tammy C.,Adam, Leonard P.,Chen, Alice Ye A.,Taylor, David S.,Yang, Richard Z.,Zhuang, Shaobin,Sleph, Paul G.,Li, Julia P.,Li, Danshi,Yin, Xiaohong,Chang, Ming,Chen, Xue-Qing,Shen, Hong,Li, Jianqing,Smith, Daniel,Wu, Dauh-Rurng,Leith, Leslie,Harikrishnan, Lalgudi S.,Kamau, Muthoni G.,Miller, Michael M.,Bilder, Donna,Rampulla, Richard,Li, Yi-Xin,Xu, Carrie,Lawrence, R. Michael,Poss, Michael A.,Levesque, Paul,Gordon, David A.,Huang, Christine S.,Finlay, Heather J.,Wexler, Ruth R.,Salvati, Mark E.
p. 9010 - 9026
(2015/12/09)
Synthesis of tertiary carbinamines
An efficient synthesis of tertiary carbinamines using a one-pot, three-component reaction employing TMSCl activation of an intermediate imine salt followed by addition of an organometallic is described. An optimized second generation chiral synthesis of select tertiary carbinamines utilizing the Ellman sulfinamine was subsequently developed on a multi-gram scale and is also described.
Kamau, Muthoni G.,Harikrishnan, Lalgudi S.,Finlay, Heather J.,Qiao, Jennifer X.,Jiang, Ji,Poss, Michael A.,Salvati, Mark E.,Wexler, Ruth R.,Lawrence, R. Michael
p. 2696 - 2703
(2012/04/17)
HETEROCYCLIC CETP INHIBITORS
Compounds of formula Ia and Ib wherein A, B, C and R1 are described herein.
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Page/Page column 349-350
(2010/11/27)
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