通过苯并呋喃氧化去芳构化级联反应实现 Integrastatin B 的全合成。
Total Synthesis of Integrastatin B Enabled by a Benzofuran Oxidative Dearomatization Cascade.
机构信息
Division of Organic Chemistry, CSIR-National Chemical Laboratory , Dr. Homi Bhabha Road, Pune 411008, India.
出版信息
Org Lett. 2016 Mar 18;18(6):1458-61. doi: 10.1021/acs.orglett.6b00404. Epub 2016 Mar 7.
PMID:26950641
Abstract
The first total synthesis of integrastatin B, a potent HIV-1 integrase inhibitor, has been accomplished in seven steps with a 17.9% overall yield employing easily accessible starting compounds. The Oxone-mediated oxidative benzofuran dearomatization cascade has been employed as the key skeletal construct to forge the central tetracyclic nucleus.
摘要
已通过 7 步反应以 17.9%的总收率完成了强效 HIV-1 整合酶抑制剂集成他汀 B 的首次全合成，采用的起始原料易得。该合成采用 Oxone 介导的苯并呋喃氧化去芳构化级联反应作为关键的骨架构建模块来构建中环的四环核心。
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