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通过 1,5-氢化物转移/7-环化级联反应实现多环吲哚氮杂卓和吲哚二氮杂卓的底物控制发散合成。

Substrate-controlled divergent synthesis of polycyclic indoloazepines and indolodiazepines via 1,5-hydride shift/7-cyclization cascades.

机构信息

State Key Laboratory of Fine Chemicals, School of Pharmaceutical Science and Technology, Dalian University of Technology, Dalian 116024, P. R. China.

出版信息

Chem Commun (Camb). 2018 Jul 12;54(57):7928-7931. doi: 10.1039/c8cc03804j.

Abstract

Novel and practical acid-catalyzed cyclization of 2-indolyl aryl carbinols via tandem dehydration/1,5-hydride shift/7-cyclization sequences has been developed. By appropriate variation of the substrate, diverse polycyclic-fused indoles were synthesized in good yield, thus demonstrating the high efficiency, transition-metal-free nature, and high step/atom economy of the synthesis strategy.

摘要

新型实用的酸催化 2-吲哚基芳基甲醇的串联脱水/1,5-氢化物转移/7-环化反应已被开发。通过适当改变底物,可以以良好的收率合成多种稠环融合的吲哚,从而证明了该合成策略的高效、无过渡金属和高步骤/原子经济性。

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