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5-HT₃受体拮抗剂盐酸阿扎司琼的合成

Synthesis of the 5-HT₃ Receptor Antagonist Azasetron Hydrochloride

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【Author】 LUO Xiao-Chuan,CHEN Guo-Hua, XU Chang-Sheng Department of Medicinal Chemistry,China Pharmaceutical University, Nanjing 210009, China

【机构】中国药科大学药化教研室；中国药科大学药化教研室南京210009；南京210009；南京210009；

【摘要】目的 :改进 5 HT3 受体拮抗剂盐酸阿扎司琼的合成工艺。方法 :以 5 氯 2 羟基苯甲酸甲酯为原料 ,经硝化、还原等九步反应合成。结果 :合成了目标化合物 ,总收率为 4 0 % ,其结构经IR ,1HNMR和MS确证。结论 :合成路线及工艺较适合于工业化生产。更多还原

【Abstract】 AIM:The purpose is to develop the general process for the synthesis of 5-HT 3 receptor antagonist Azasetron Hydrochloride. METHOD: It was synthesized from methyl 5-chloro-2-hydroxyl benzoic acid via nine-step reaction with nitration,reduction,etc. RESULT: The title compound was obtained with 40% overall yield. The structure was confirmed by IR, 1 HNMR and MS. CONCLUSION:Some improvements for the synthesis of Azasetron Hydrochloride were made.更多还原