一种5-羟基吲哚制备新工艺

介绍了一种以吲哚为原料合成5-羟基吲哚的新方法。该方法采用磺酸基保护吲哚活泼3位,取代吲哚5位获得了5-溴吲哚,经水解合成目标物。本方法首次采用相转移催化剂实现了5-溴吲哚得高效率水解。优化了合成工艺：反应物乙酸酐与2-磺酸钠-二氢吲哚一水合物的摩尔配比为20∶1,pH为11,选用四甲基氯化铵相转移催化剂,产物得率达到了81.2%。

A New Technology for the Synthesis of 5-hydroxyl Indole

Indole was prepared from 5-Hydroxyl indole.The third position on the ring of indole was protected by reaction with the group of sulfonic acid.Then 5-bromine indole was synthesized from the indole derivative.At last the target was synthesised by the reaction of hydrolysis. Phase transfer catalyst was used to the hydrolysis of 5-bromine indole first.The optimum conditions were： the reactant ratio of Acetic anhydride to 2-sulfonic acid sodium indole was 20 ∶1,pH was 11,pHase transfer catalyst was Tetramethyl ammonium chloride,and the yield was 81.2 %.