一锅法合成 1-(三氟甲基)-4-氟-1,2-二氢异喹啉和 4,4-二氟-1,2,3,4-四氢异喹啉。

One-pot synthesis of 1-(trifluoromethyl)-4-fluoro-1,2-dihydroisoquinolines and 4,4-difluoro-1,2,3,4-tetrahydroisoquinolines.

机构信息

State Key Laboratory of Organometallic Chemistry, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences , 345 Lingling Road, Shanghai 200032, China.

出版信息

Org Lett. 2013 Dec 20;15(24):6210-3. doi: 10.1021/ol403059z. Epub 2013 Nov 21.

DOI:10.1021/ol403059z

PMID:24261675

Abstract

A cascade approach to 1-(trifluoromethyl)-4-fluoro-1,2-dihydroisoquinolines and 4,4-difluorotetrahydroisoquinolines has been developed. The procedure involves a silver-catalyzed intramolecular aminofluorination of alkyne. This one-pot reaction provides an efficient way to synthesize various fluorinated isoquinolines.

摘要

一种级联方法被开发用于合成 1-(三氟甲基)-4-氟-1,2-二氢异喹啉和 4,4-二氟四氢异喹啉。该方法涉及银催化的炔烃分子内氨基氟化反应。该一锅反应为合成各种氟化异喹啉提供了一种有效的方法。