Palladium-catalyzed nucleomethylation of alkynes for synthesis of methylated heteroaromatic compounds

被引：13

作者：

Yang, Xi ^{[1
]}

Wang, Gang ^{[1
]}

Ye, Zhi-Shi ^{[1
]}

机构：

[1] Dalian Univ Technol, Zhang Dayu Sch Chem, Dalian 116024, Peoples R China

来源：

CHEMICAL SCIENCE | 2022年 / 13卷 / 34期

基金：

中国国家自然科学基金;

关键词：

C-H FUNCTIONALIZATION; ARYLBORONIC ACIDS; RECENT PROGRESS; ARYL HALIDES; INDOLES; ALKYLATION; REAGENTS; BOND; GRIGNARD; METHYLALUMINUM;

D O I：

10.1039/d2sc03294e

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

Herein, we disclosed a novel and efficient palladium-catalyzed nucleomethylation of alkynes for the simultaneous construction of the heteroaromatic ring and methyl group. The 3-methylindoles, 3-methylbenzofurans and 4-methylisoquinolines were obtained in moderate to excellent yields. Notably, this methodology was employed as a key step for synthesis of a pregnane X receptor antagonist, zindoxifene, bazedoxifene and AFN-1252. The kinetic studies revealed that reductive elimination might be the rate-determining step.

引用

页码：10095 / 10102

页数：8

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