中枢性降压药莫索尼定的合成工艺

Synthesis of the Secondary Generation of Central Hypotensor Moxonidine

以乙脒盐酸盐为原料 ,经环合硝化、氯化、还原、加成脱水、醇解成盐合成了中枢性降压药莫索尼定 ,总产率为 2 4 8%。在氯化反应中 ,以三氯氧磷为氯化剂 ,产率为 92 8%。在还原反应中 ,以铁粉为还原剂 ,完成反应后进行水蒸气蒸馏 ,产率为 87 7%。

Moxonidine is known as the central hypotensor of the secondary generation.It was synthesized from acetamidine hydrochloride as the starting material via cyclization,nitration,chlorination,reduction,addition and dehydration,alcoholysis and salt formation.The overal yield was 24 8%.The yield of chlorination was 92 8%,using phosphorus oxychloride as the chlorinating agent.The yield of reduction was 87 7%,using iron powder as the reducting agent and steam distillation as the separation method.