Solid-phase and solution-phase parallel synthesis of tetrahydroisoquinolines via Pictet-Spengler reaction

被引：16

作者：

Sun, Q ^{[1
]}

Kyle, DJ ^{[1
]}

机构：

[1] Purdue Pharm LP, Dept Computat Combinatorial & Med Chem, Cranbury, NJ 08512 USA

来源：

COMBINATORIAL CHEMISTRY & HIGH THROUGHPUT SCREENING | 2002年 / 5卷 / 01期

关键词：

D O I：

10.2174/1386207023330624

中图分类号：

Q5 [生物化学];

学科分类号：

071010 ; 081704 ;

摘要：

An efficient parallel synthesis of 6,7-dimethoxytetrahydroisoquinolines is reported. The key reaction step is 3,4-dimethoxyphenethylimines reacting with acid chlorides to form an N-acyliminium ion intermediate, which undergoes Pictet-Spengler condensation to give the desired products in >80% yield. Both solution-phase and solid-phase synthesis of 6,7-dimethoxytetrahydroisoquinolines are described.

引用

页码：75 / 81

页数：7

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