布南色林关键中间体的合成

目的合成布南色林的关键中间体。方法布南色林为新的治疗精神分裂症药物,本文归纳了其合成方法,并提出了一种新的关键中间体合成方法:由对氟苯甲酸乙酯与乙酰乙酸乙酯反应得对氟苯甲酰乙酸乙酯,再经氨解制得3-(4-氟苯基)-3-氧代丙酰胺,然后与环辛酮环合得到4-(4-氟苯基)-5,6,7,8,9,10-六氢环辛烷并[b]吡啶-2(1H)-酮。结果用新方法合成了布南色林的关键中间体,总收率57.6%。结论该路线反应条件温和,适合工业化生产。

Synthesis of the key intermediate of Blonanserin

Objective To synthesis the key intermediate of Blonanserin.Methods Blonanserin was a new antipsychotic drug.In this paper,author summarized the synthesies of Blonanserin and proposed a new synthetic method of the key intermediate referring to literatures.The reaction of ethyl 4-fluorobenzoate with ethyl acetoacetate can generate 4-fluorobenzoylacetic acid ethyl ester,and then prepared 3-(4-fluorophenyl)-3-oxopropanamide by ammonolysis,followed by the cyclization with cyclooctanone,obtained 4-(4-fluorophenyl...