Asymmetric synthesis of chiral heterobenzylic amines via visible-light-induced enantioselective C(sp3)-H alkylation

Yumei Huo , Beibei Chen , Xiaoyu Ren , Chao Wang , Rupeng Qi , Zhaoqing Xu
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Abstract

The chiral heterobenzylic amines, such as α-alkyl substituted chiral oxadiazole methylamine skeletons are widely present in pesticides and pharmaceuticals, due to their unique biological activities. The enantioselective C(sp3)-H alkylation of heterobenzylic amines is an important strategy for the synthesis of α-alkylate chiral heterobenzylic amines. Herein, we disclose the first example of photoinduced and Cu-catalyzed enantioselective decarboxylative C(sp3)-H alkylation of oxadiazole methylamines.

Abstract Image

Abstract Image

可见光诱导对映选择性C(sp3)-H烷基化不对称合成手性杂酶胺
α-烷基取代手性恶二唑甲胺骨架等手性杂酶胺因其独特的生物活性而广泛存在于农药和医药中。杂酶胺的对映选择性C(sp3)-H烷基化反应是合成α-烷基化手性杂酶胺的重要策略。在此,我们公开了光诱导和铜催化的恶二唑甲胺的对映选择性C(sp3)-H烷基化的第一个例子。
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CiteScore
14.40
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