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盐酸苯达莫司汀的合成 被引量:2

Synthesis of Bendamustine Hydrochloride
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摘要 以2,4-二硝基氯苯为起始原料,依次经甲胺化,选择性还原,N-酰化,环合,催化氢化,N-二羟乙基化,O-甲磺酰化,氯置换,酸化水解和成盐等10步反应合成盐酸苯达莫司汀,其结构经~1H NMR确证,总收率48.4%,纯度99.5%。 Bendamustine hydrochloride was synthesized by a ten-step reaction of amination,selective reduction,N-acylation,cyclization,catalytic hydrogenation,hydroxyethylation,O-sulfonylation,chlorination,hydrolysis and salification,using 2,4-dinitrochlorobenzen as starting material. The structure was confirmed by^1 H NMR. The total yield and purity were 48. 4% and 99. 5%,respectively.
出处 《合成化学》 CAS CSCD 2016年第5期457-460,共4页 Chinese Journal of Synthetic Chemistry
基金 国家自然科学基金资助项目(21476078 20972051) 上海市科技支撑计划(12431900900 12431900902)
关键词 2 4-二硝基氯苯 苯达莫司汀 药物合成 工艺改进 2 4-dinitrochlorobenzen bendamustine drug synthesis process improvement
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