Synthesis of tetrahydroisoquinolines through TiCl4-mediated cyclization and Et3SiH reduction  

作　　者：Zeyu Shi Qiong Xiao Dali Yin 

机构地区：[1]State Key Laboratory of Bioactive Substances and Functions of Natural Medicines,Institute of Materia Medica,Peking Union Medical College and Chinese Academy of Medical Sciences,Beijing 100050,China [2]Department of Medicinal Chemistry,Beijing Key Laboratory of Active Substances Discovery and Drugability Evaluation,Institute of Materia Medica,Peking Union Medical College and Chinese Academy of Medical Sciences,Beijing 100050,China

出　　处：《Chinese Chemical Letters》2020年第3期729-732,共4页中国化学快报（英文版）

基　　金：financial support from Drug Innovation Major Project(No.2018ZX09711-001-005);CAMS Collaborative Innovation Project(No.2017-I2M-2-004)。

摘　　要：A versatile and efficient telescoped reaction sequence for the synthesis of tetrahydroisoquinolines(THIQs)is reported that uses TiCl4 to promote cyclization of a benzylaminoacetal derivative and Et3SiH for reduction of the intermediate 4-hydroxy-THIQ.This method is complimentary to the classical Pomeranz-Fritsch and related reactions since it tolerates electron-withdrawing substituents and allows access to 8-substituted THIQs.

关 键 词：TETRAHYDROISOQUINOLINE TICL4 CYCLIZATION Et3SiH Telescoped REACTION 

分 类 号：O626[理学—有机化学]