奥沙米特合成工艺的研究

Studies on synthesis of oxatomide

以邻苯二胺为起始原料 ,经 4步反应合成了H1 组胺受体拮抗剂奥沙米特。作者研究了 4步反应的工艺条件 ,如合成化合物 5时 ,改变二苯甲醇与无水哌嗪的投料比 ;合成化合物 4时 ,文献缩合剂为氢氧化钾和相转移催化 ,改为乙醇钠为缩合剂 ;合成化合物 1时 ,溶剂由甲苯改为DMF 。

Oxatomide was synthesized from o phenylenediamine with four improved steps. Compound 5 was synthesized in an improved ratio of diphenylmethanol and anhydrous piperazine. Compound 4 was synthesized with an improved condensing agent. Compound 1 was synthesized with an improved solvent. The yield of every step was increased.