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 o...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.展开更多
基金financial support from Drug Innovation Major Project(No.2018ZX09711-001-005)CAMS Collaborative Innovation Project(No.2017-I2M-2-004)。
文摘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.
基金supported by the National Natural Science Foundation of China(U1205112,51002053)Key Project of the Ministry of Education of China(212206)+2 种基金Program for Prominent Young Talents in Fujian Province University,ChinaProgram for New Century Excellent Talents in Fujian Province University,ChinaPromotion Program for Yong and Middle-aged Teacher in Science and Technology Research of Huaqiao University,China(ZQN-YX102)~~