CAJ | 학술논문

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。
염산분체막사정시용우치료만성림파세포성백혈병( CLL)급유선암적약물,시장전경엄활[1]。목전적합성방법중존재반응조건가각、산솔저등결점。본문이2,4-이초기록분위원료,통과취대、환원、선화、배합、최화환원、경기화、성염등칠보반응성공합성염산분체막사정,종산솔위40．99%。반응조건온화、보취소,강저료생산성본이급설비요구,유량호적공업화응용전경。
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.