期刊
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY
卷 140, 期 46, 页码 15976-15984出版社
AMER CHEMICAL SOC
DOI: 10.1021/jacs.8b10564
关键词
-
资金
- National Institutes of Health [GM058160-17S1]
- NATIONAL INSTITUTE OF GENERAL MEDICAL SCIENCES [R01GM058160, R35GM122483] Funding Source: NIH RePORTER
A mild and practical method for the catalytic installation of the amino group across alkenes and alkynes has long been recognized as a significant challenge in synthetic chemistry. As the direct hydroamination of olefins using ammonia requires harsh conditions, the development of suitable electrophilic aminating reagents for formal hydroamination methods is of importance. Herein, we describe the use of 1,2-benzisoxazole as a practical electrophilic primary amine source. Using this heterocycle as a new amino group delivery agent, a mild and general protocol for the copper-hydride-catalyzed hydroamination of alkenes and alkynes to form primary amines was developed. This method provides access to a broad range of chiral alpha-branched primary amines and linear primary amines, as demonstrated by the efficient synthesis of the antiretroviral drug maraviroc and the formal synthesis of several other pharmaceutical agents.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据