21604-47-7Relevant articles and documents
Regioselective Synthesis of Multifunctional Allylic Amines; Access to Ambiphilic Aziridine Scaffolds
McLaughlin, Mark G.,Roberts, Dean D.
supporting information, p. 4463 - 4467 (2021/06/28)
We describe, for the first time, a highly regioselective hydrosilylation of propargylic amines. The reaction utilizes a PtCl2/XantPhos catalyst system to deliver hydrosilanes across the alkyne to afford multifunctional allylic amines in high yields. The reaction is tolerant to a wide variety of functional groups and provides high value intermediates with two distinct functional handles. The synthetic applicability of the reaction has been shown through the synthesis of diverse ambiphilic aziridines.
CuI-catalyzed cycloisomerization of propargyl amides
Alhalib, Ali,Moran, Wesley J.
, p. 795 - 800 (2014/01/23)
The synthesis of substituted dihydrooxazoles by the CuI-catalyzed cycloisomerization of terminal propargyl amides is reported. The reaction has been shown to have good substrate scope and experiments to delineate the mechanism have been performed. Substrates containing a benzylic methylene were oxidized to the ketone under the reaction conditions.
The synthesis and structure-activity relationship studies of selective acetyl-CoA carboxylase inhibitors containing 4-(thiazol-5-yl)but-3-yn-2-amino motif: Polar region modifications
Xu, Xiangdong,Weitzberg, Moshe,Keyes, Robert F.,Li, Qun,Wang, Rongqi,Wang, Xiaojun,Zhang, Xiaolin,Frevert, Ernst U.,Camp, Heidi S.,Beutel, Bruce A.,Sham, Hing L.,Gu, Yu Gui
, p. 1803 - 1807 (2007/10/03)
The structure-activity relationship study focused on the polar region of the HTS hit A-80040 (1) producing several series of potent and selective ACC2 inhibitors. The SAR suggests a compact lipophilic pocket that does not tolerate polar and ionic groups.
