强碱性条件下的相转移催化合成美多心安

PHASE TRANSFER CATALYZED SYNTHESIS OF METOPROLOL IN CONDITION OF STRONG ALKALI

以对甲氧乙基苯酚和环氧氯丙烷为原料,强碱KOH为催化剂,PEG400(聚乙二醇400)为相转移催化剂,通过醚化反应和胺化反应合成了美多心安。本工艺路线简单,原料易得,反应的整体收率达到50%。研究了不同反应条件对反应的影响。对中间体和目标产物进行了IR、1HNMR、HPLC定性定量分析。确定了较好的合成反应条件。

This paper has studied strong alkali catalyst KOH and phase transfer catalyst PEG400 in synthesizing Metoprolol by 4 - （2 - methoxy - ethyl） phenol and epichlorohydrin by etherification reaction and amination reaction. The technics of the synthesis is original , the raw materials were easy to be acquired, the route is easy, The yield of product is 50%. The effects of differents reaction conditions were studied. The composition of intermediate and products were examined by IR and 1HNMR method. The appropriate reaction condition were established.