Copper-Mediated N-Cyclopropylation of Azoles, Amides, and Sulfonamides by Cyclopropylboronic Acid
摘要:
Reaction of azoles, amides, and sulfonamides in dichloroethane with readily available cyclopropylboronic acid in the presence of copper acetate and sodium carbonate afforded the N-cyclopropyl derivatives in good to excellent yields.
The present invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. Compounds of the invention inhibit, regulate and/or modulate kinases, particularly Tie-2. Methods of using the compounds and pharmaceutical compositions thereof to treat kinase-dependent diseases and conditions are also an aspect of the invention.
Palladium-Catalyzed α-Arylation of 2-Chloroacetates and 2-Chloroacetamides
作者:Gary A. Molander、Kaitlin M. Traister、Thiago Barcellos
DOI:10.1021/jo400488q
日期:2013.4.19
A method has been developed for the Pd-catalyzed synthesis of alpha-(hetero)aryl esters and amides through a Suzuki-Miyaura cross-coupling reaction. This method avoids the use of strong base, does not necessitate inert or low temperature formation of reagents, and does not require the use of a large excess of organometallic reagent. Utilization of organotrifluoroborate salts as nucleophilic partners allows a variety of functional groups and heterocyclic compounds to be tolerated.
US8178570B2
申请人:——
公开号:US8178570B2
公开(公告)日:2012-05-15
Copper-Mediated <i>N</i>-Cyclopropylation of Azoles, Amides, and Sulfonamides by Cyclopropylboronic Acid
作者:Sébastien Bénard、Luc Neuville、Jieping Zhu
DOI:10.1021/jo801033y
日期:2008.8.1
Reaction of azoles, amides, and sulfonamides in dichloroethane with readily available cyclopropylboronic acid in the presence of copper acetate and sodium carbonate afforded the N-cyclopropyl derivatives in good to excellent yields.