盐酸苯达莫司汀是用于治疗慢性淋巴细胞性白血病( CLL)及乳腺癌的药物,市场前景广阔[1]。目前的合成方法中存在反应条件苛刻、产率低等缺点。本文以2,4-二硝基氯苯为原料,通过取代、还原、酰化、环合、催化还原、烃基化、成盐等七步反应成功合成盐酸苯达莫司汀,终产率为40．99%。反应条件温和、步骤少,降低了生产成本以及设备要求,有良好的工业化应用前景。%Bendamustine hydrochloride,a derivant of nitrogen mustard,is a bioalkylating agengt,essentially used for the treatment of chronic lymphocytic leukemia and lymphomas. The process for its preparation generally suffers from the drawback of a high require of reaction condition. The synthetic process of bendamustine hydrochloride through seven main reactions,such as substitution,reduc-tion,acylation,cyclization,reduction,alkylation,salification reaction etc was reported in this paper. A short synthesis route with mild reaction conditions,less steps,reducing the production cost and equipment requirements,a good prospect of industrialization,was provided.
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