利托君的合成

Synthesis of Ritodrine

苯酚和丙酰氯经酯化及Fries重排得到对羟基苯丙酮,经溴化铜溴代所得α-溴对羟基苯丙酮,在THF中与对羟基苯乙胺进行缩合、硼氢化钾还原,制得抗早产药利托君,总收率约39%。

p-Hydroxypropiophenone, which was synthesized from phenol and propionyl chloride by esterification and Fries rearrangement reaction, reacted with CuBr2 to obtain α-bromo-p-hydroxypropiophenone, followed by the condensation with p-hydroxyphenethylamine in THF and reduction with KBH4 to give ritodrine. The overall yield was about 39 %.