【摘要】 目的:研究三光气法合成盐酸布比卡因。方法:以三光气作为氯化剂,由2-哌啶甲酸经酰氯化、酰胺化、丁基化、成盐得盐酸布比卡因。结果:盐酸布比卡因合成总收率为42.9%。合成反应条件温和,选择性好,得到的中间体可直接用于后续反应。结论:本方法操作简单,污染少,适合工业化生产。更多还原

【Abstract】 Objective: To study the synthesis of Bupivacaine hydrochloride by triphosgene.Methods: Bupivacaine hydrochloride was prepared via chlorination by triphosgene,amidation,butylation and acidification from 2-pipecolic acid.Results: The overall yield was 42.9%.The reactions were carried out under moderate condition with good selectivity.The intermediate can be directly used in the next step without any more purification.Conclusion: The process is easily controlled and there is no pollution to the environment.Therefore,it is suitable for industrial manufacture.更多还原