21604-47-7Relevant academic research and scientific papers
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.
THERAPEUTIC COMPOUNDS AND USES THEREOF
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Page/Page column 91, (2016/08/23)
The present invention relates to compounds of formula (I): and to salts thereof, wherein R1-R6 have any of the values defined in the specification, and compositions and uses thereof. The compounds are useful as inhibitors of TAF1. Also included are pharmaceutical compositions comprising a compound of formula (I) or a pharmaceutically acceptable salt thereof, and methods of using such compounds and salts in the treatment of various TAF1-mediated disorders.
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.
Cyclization-carbonylation-cyclization coupling reactions of propargyl acetates and amides with palladium(II)-bisoxazoline catalysts
Yasuhara, Sumie,Sasa, Makiko,Kusakabe, Taichi,Takayama, Hiroyuki,Kimura, Masayuki,Mochida, Tomoyuki,Kato, Keisuke
supporting information; experimental part, p. 3912 - 3915 (2011/06/20)
Clever boxing: A cyclization-carbonylation-cyclization-coupling reaction of propargyl acetates 1 or amides 2 in the presence of a palladium(II)- bisoxazoline (box) catalyst afforded symmetrical ketones of types 3 and 4, respectively, containing two heterocyclic groups in moderate to excellent yields (see scheme; tfa=trifluoroacetate). Compounds 3 were converted into ketones containing two 3(2H)-furanone rings.
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.
Substituted bicyclic derivatives useful as anticancer agents
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, (2008/06/13)
The invention relates to compounds of the formula 1 and to pharmaceutically acceptable salts and solvates thereof, wherein A, X, R1, R3and R4are as defined herein. The invention also relates to methods of treating abnormal cell growth in mammals with administering the compounds of formula 1 and to pharmaceutical compositions for treating such disorders which contain the compounds of formula 1. The invention also relates to methods of preparing the compounds of formula 1.
