运用PEG相转移催化剂合成β受体阻滞剂Metoprolol酒石酸盐

Preparation of the Selective β Receptor Blocking Agent Metoprolol Tartrate with PEG Phase Transfer Catalysts

提供了一种具有应用前景的合成M etoprolol酒石酸盐新工艺.产品以对甲氧乙基苯酚和环氧氯丙烷为原料,在相转移催化剂聚乙二醇400的作用下发生缩合反应合成2-[4-(2-甲氧基乙基)苯氧基]环氧乙烷中间体,中间体再经过胺化反应合成M etoprolol,M etoprolol与酒石酸成盐生成了M etoprolol酒石酸盐.产物由红外光谱(IR)、核磁光谱(1HNMR)、物理及化学分析等方法证实与目标产物基本一致,总收率达50%.

A new process with good respects and some value in production and application has been described in this paper. The products are prepared from raw materials of 4 - （2 - methoxyethyl） phenol and epichlorohydrin. At first,the intermediate 3 - [ p - （2 - methoxyethyl） - phenoxy ] - 1,2 - epoxypropane is synthesized as by the condensation reaction with the phase transfer catalysts polyethylene glycol 400. Subsequently, the intermediate via the amined reaction is synthesizedas Metoprolol. By the salted reaction, Metoprolol with tartaric acid has been synthesized its tartrate. The structures of above - mentioned product were comfirmed by IR, ^1H NMR, physics and chemistry analysis etc to be basically consistent with those of target products. The total yield of product is 50%.