102684-91-3Relevant articles and documents
Mechanistic studies of copper(I)-catalyzed 1,3-halogen migration
Van Hoveln, Ryan,Hudson, Brandi M.,Wedler, Henry B.,Bates, Desiree M.,Le Gros, Gabriel,Tantillo, Dean J.,Schomaker, Jennifer M.
supporting information, p. 5346 - 5354 (2015/05/13)
An ongoing challenge in modern catalysis is to identify and understand new modes of reactivity promoted by earth-abundant and inexpensive first-row transition metals. Herein, we report a mechanistic study of an unusual copper(I)-catalyzed 1,3-migration of 2-bromostyrenes that reincorporates the bromine activating group into the final product with concomitant borylation of the aryl halide bond. A combination of experimental and computational studies indicated this reaction does not involve any oxidation state changes at copper; rather, migration occurs through a series of formal sigmatropic shifts. Insight provided from these studies will be used to expand the utility of aryl copper species in synthesis and develop new ligands for enantioselective copper-catalyzed halogenation.
DP2 Antagonist and Uses Thereof
-
Page/Page column 31, (2011/02/26)
Described herein is the DP2 antagonist [2′-(3-benzyl-1-ethyl-ureidomethyl)-6-methoxy-4′-trifluoromethyl-biphenyl-3-yl]-acetic acid, or a pharmaceutically acceptable salt thereof. Also described are methods of preparing the DP2 antagonist, or a
Discovery of INCB9471, a potent, selective, and orally bioavailable CCR5 antagonist with potent anti-HIV-1 activity
Xue, Chu-Biao,Chen, Lihua,Cao, Ganfeng,Zhang, Ke,Wang, Anlai,Meloni, David,Glenn, Joseph,Anand, Rajan,Xia, Michael,Kong, Ling,Huang, Taisheng,Feng, Hao,Zheng, Changsheng,Li, Mei,Galya, Laurine,Zhou, Jiacheng,Shin, Niu,Baribaud, Fredric,Solomon, Kim,Scherle, Peggy,Zhao, Bitao,Diamond, Sharon,Emm, Tom,Keller, Douglas,Contel, Nancy,Yeleswaram, Swamy,Vaddi, Kris,Hollis, Gregory,Newton, Robert,Friedman, Steven,Metcalf, Brian
scheme or table, p. 483 - 487 (2011/03/20)
To identify a CCR5 antagonist as an HIV-1 entry inhibitor, we designed a novel series of indane derivatives based on conformational considerations. Modification on the indane ring led to the discovery of compound 22a (INCB9471) that exhibited high affinit