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钯催化喹诺酮衍生物通过脱羧C-S交叉偶联进行硫醚化反应

Palladium-Catalyzed Thioetherification of Quinolone Derivatives via Decarboxylative C-S Cross-Couplings.

作者信息

Xia Chengcai, Wei Zhenjiang, Yang Yong, Yu Wenbo, Liao Hanxiao, Shen Chao, Zhang Pengfei

机构信息

College of Material, Chemistry and Chemical Engineering, Hangzhou Normal University, Hangzhou, 310036, China.

Pharmacy College, Zhejiang University of Technology, Hangzhou, 310014, China.

出版信息

Chem Asian J. 2016 Feb 4;11(3):360-6. doi: 10.1002/asia.201500808. Epub 2015 Oct 23.

Abstract

A highly efficient and practical procedure for palladium-catalyzed direct thioetherification of quinolone derivatives with diaryl disulfides through decarboxylative C-S coupling has been established. The reaction could proceed smoothly under air in the presence of Pd(OAc)2 and Ag2 CO3 in DMSO. This protocol provides an appealing alternative to existing approaches to construct aryl sulfides of quinolone derivatives, which may be used as key intermediates in the synthesis of drug candidates.

摘要

已建立了一种高效实用的方法,通过脱羧C-S偶联实现钯催化喹诺酮衍生物与二芳基二硫化物的直接硫醚化反应。该反应在空气中,于二甲基亚砜(DMSO)中,在醋酸钯(Pd(OAc)₂)和碳酸银(Ag₂CO₃)存在下可顺利进行。该方案为构建喹诺酮衍生物芳基硫化物的现有方法提供了一种有吸引力的替代方法,这些芳基硫化物可用作候选药物合成中的关键中间体。

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