四氢异喹啉衍生物的合成研究

Synthesis of 1,2,3,4-Tetrahydroisoquinoline Derivatives

以间甲氧基苯乙胺和氯甲酸乙酯为原料,通过亲核取代、关环、铝锂氢还原、脱甲基以及在N位上Boc保护及脱保护等9步反应得到一系列重要的1,2,3,4-四氢异喹啉及其衍生物.产物的结构经核磁共振氢谱、红外光谱及元素分析确证.与传统四氢异喹啉衍生物的合成工艺相比,该工艺反应条件温和、简便、经济、产率高且对环境友好.

A series of important 1,2,3,4-tetrahydroisoquinoline derivatives were synthesized from 2-（3-methoxyphenyl）ethylamine and ethyl chloroformate by nucleophilic substitution, cyclization, LiA1H4 reduction and other reactions amounting to 9 steps. The structures of the products were characterized by IR, 1H NMR spectra and elemental analysis. Compared to the traditional synthetic procedures of tetrahydroisoquinoline, our procedures were temperate, convenient, economical, high-yielding and environment- friendly.