几个简单,快速和实用的协议已被开发来合成内部或末端炔丙胺和查耳酮通过甲3 -耦合醛,胺的反应,和炔由容易获得的催化剂催化的Ag 2 CO 3无溶剂条件下进行。反应进行得很顺利,以良好的收率和良好的官能团耐受性提供了各种产品。已经证明了克级制备,生物活性分子合成和不对称底物。此外,已经提出了合成不同产物的合理机制。
Facile and Selective Synthesis of Propargylic Amines and 1,6-Diynes: One-Pot Three-Component Coupling Reactions of Alkynylsilanes, Aldehydes and Amines by a Cooperative Catalytic System Comprised of CuCl and Cu(OTf)<sub>2</sub>
作者:Norio Sakai、Naoki Uchida、Takeo Konakahara
DOI:10.1055/s-2008-1077790
日期:2008.6
Described herein is a three-component coupling reaction of alkynylsilanes, aldehydes and amines by a cooperative catalytic system comprised of CuCl and Cu(OTf)(2), leading to the production of a variety of propargyl amine derivatives. This catalytic system was successfully applied to the practical preparation of 1,6-diyne derivatives via twice-performed, domino-type coupling reactions.
Ag2CO3-catalyzed efficient synthesis of internal or terminal propargylicamines and chalcones via A3-coupling under solvent-free condition
or terminal propargylamines and chalcones via A3-coupling reaction of aldehydes, amines, and alkynes catalyzed by an easily available catalyst Ag2CO3 under solvent-free condition. The reaction proceeded smoothly to deliver various products in good-to-excellent yields with good functional group tolerance. Gram-scale preparation, bioactive molecule synthesis and asymmetric substrates have been demonstrated
几个简单,快速和实用的协议已被开发来合成内部或末端炔丙胺和查耳酮通过甲3 -耦合醛,胺的反应,和炔由容易获得的催化剂催化的Ag 2 CO 3无溶剂条件下进行。反应进行得很顺利,以良好的收率和良好的官能团耐受性提供了各种产品。已经证明了克级制备,生物活性分子合成和不对称底物。此外,已经提出了合成不同产物的合理机制。