石杉碱甲关键中间体的合成

Synthesis of a Key Intermediate of Huperzine A

目的,研究石杉碱甲关键中间体β-酮酯的合成路线及工艺;方法,以7,8-二氢-1-甲氧基萘(1)为起始原料,经羰基化反应、环氧化物异构化、双环环化得β-酮酯,总收率8.5%;结果,合成了目标化合物,其化学结构经元素分析、IR、1HNMR、13CNMR、MS得以确证;结论,该合成路线及工艺使石杉碱甲关键中间体β-酮酯的收率提高了,并降低了成本。

[AIM]To study an improved process for the preparation of a Key Intermediate β-Keto ester of Huperzine A （6）. [METHODS]Compound （1）was synthesized from 7,8-Dihydro-2- hydroxynaphthalene （1）by carbonylation reaction, an epoxide isomerization and a bicycloannulation reaction.The overall yield was 8.5% . [RESULTS]The constitution of （6） was confirmed by elemental analysis,IR, 1HNMR, 13CNMR, MS.[CONCLUSION] This synthesis improve the yield,and reduce costs of β-Keto ester.