2-羟基-3,4,6-三甲氧基查尔酮的合成

Synthesis of 2-Hydroxy-3,4,6-trimethoxychalcone

本文开发了一种天然产物2-羟基-3,4,6-三甲氧基查尔酮(1)的十克级规模快速合成方法。通过改良合成2-羟基-3,4,6-三甲氧基苯甲醛(7)的甲基化和甲酰化条件,将7的合成总收率从文献报道的22%提高至68%。并以7为原料在乙腈为溶剂、80℃加热的条件下通过Wittig反应在50mmol规模以85%的收率合成了产物1。

A convenient 10-grams-scale synthesis of 2-hydroxy-3,4,6-trimethoxychalcone(1)is described.The total yield of 2-hydroxy-3,4,6-trimethoxybenzaldehyde(7)was increased from 22%reported in the literature to 68%after the optimization of methylation and formylation.1 was furnished in 85%yield at 80℃from 7 via the Wittig reaction in acetonitrile.