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钯催化的由可去除 Bts 保护基导向的胺的γ-C(sp3)-H 键乙酰化反应。

Pd-Catalyzed Acetoxylation of γ-C(sp)-H Bonds of Amines Directed by a Removable Bts-Protecting Group.

机构信息

State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences , 501 Haike Road, Shanghai 201203, China.

出版信息

J Org Chem. 2018 Feb 16;83(4):2448-2454. doi: 10.1021/acs.joc.7b02995. Epub 2018 Feb 6.

Abstract

Pd-catalyzed acetoxylation of γ-C(sp)-H bonds directed by Bts-protected amines using inexpensive PhI(OAc) as oxidant is reported. The Bts-protecting group is easily introduced and removed under mild conditions. This protocol provides an important strategy for the construction of γ-hydroxyl amine derivatives.

摘要

Pd 催化的 Bts 保护胺导向的γ-C(sp)-H 键乙酰化反应,使用廉价的 PhI(OAc)作为氧化剂。Bts 保护基在温和条件下可方便地引入和去除。该方案为γ-羟基胺衍生物的构建提供了重要策略。

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