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中枢性降压药莫索尼定的合成工艺
引用本文:武引文,梅和珊,张忠敏,吕新英,颜廷仁. 中枢性降压药莫索尼定的合成工艺[J]. 中国药物化学杂志, 2001, 11(1): 45-46
作者姓名:武引文  梅和珊  张忠敏  吕新英  颜廷仁
作者单位:1. 河北医科大学药学院,河北 石家庄 050017
2. 河北省灵寿县中学,河北 灵寿 050500
摘    要: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24.8%。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%。

关 键 词:莫索尼定;合成;硝化;还原
文章编号:1005-0108(2001)01-0045-02
修稿时间:2000-08-28

Synthesis of the SecondaryGeneration of Central Hypotensor Moxonidine
WU Yin wen ,MEI He shan ,ZHANG Zhong min ,LU XIN ying ,YAN Ting ren. Synthesis of the SecondaryGeneration of Central Hypotensor Moxonidine[J]. Chinese Journal of Medicinal Chemistry, 2001, 11(1): 45-46
Authors:WU Yin wen   MEI He shan   ZHANG Zhong min   LU XIN ying   YAN Ting ren
Affiliation:WU Yin wen 1,MEI He shan 1,ZHANG Zhong min 1,LU XIN ying 2,YAN Ting ren 1
Abstract: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.
Keywords:moxonidine  synthesis  nitration  reduction
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