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4-烷基异喹啉-1,3(2,4)-二酮衍生物的对映选择性胺化反应

Enantioselective amination of 4-alkylisoquinoline-1,3(2,4)-dione derivatives.

作者信息

Cheng Cheng, Li Ying-Xian, Jia Xue-Min, Zhang Ji-Quan, Zhao Yong-Long, Feng Wei, Tang Lei, Yang Yuan-Yong

机构信息

State Key Laboratory of Functions and Applications of Medicinal Plants, Guizhou Provincial Engineering Technology Research Center for Chemical Drug R&D, School of Pharmacy, Guizhou Medical University Guiyang 550004 China

BGI-Shenzhen Building 11, Beishan Industrial Zone, Yantian Shenzhen 518083 China.

出版信息

RSC Adv. 2020 Nov 25;10(70):42912-42915. doi: 10.1039/d0ra07806a. eCollection 2020 Nov 23.

Abstract

A mild and efficient enantioselective amination of 4-alkylisoquinoline-1,3(2,4)-dione derivatives was established, which is compatible with a broad range of substrates and delivers the final products in excellent yields (up to 99%) and ee values (up to 99%) with low catalyst loading (down to 1 mol%). The synthetic potential of this methodology was also demonstrated in the gram scale level.

摘要

建立了一种温和且高效的4-烷基异喹啉-1,3(2,4)-二酮衍生物的对映选择性胺化反应,该反应与多种底物兼容,能以低催化剂负载量(低至1 mol%)、优异的产率(高达99%)和对映体过量值(高达99%)得到最终产物。该方法的合成潜力也在克级规模上得到了证明。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7666/9058008/7c02d2fc04a0/d0ra07806a-f1.jpg

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