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盐酸西替克新合成工艺改进
引用本文:赵明明,李颖,李岩松,宋宏锐.盐酸西替克新合成工艺改进[J].精细化工中间体,2010,40(3):34-36.
作者姓名:赵明明  李颖  李岩松  宋宏锐
作者单位:沈阳药科大学,制药工程学院,辽宁,沈阳,110016
摘    要:以L-胱氨酸为原料,通过氯甲酸苄酯保护2个氨基,之后用五氯化磷氯代,再与溴己新反应,最后用盐酸乙醇溶液成盐.生成盐酸西替克新。目标产物盐酸西替克新的结构经LC-MS、IR、1HNMR谱确证,该合成方法工艺路线简单,收率可达40.0%。

关 键 词:盐酸西替克新  药物化学  工艺改进  祛痰药

Improved Synthesis of Cistinexine Hydrochloride
ZHAO Ming-ming,LI Ying,LI Yan-song,SONG Hong-rui.Improved Synthesis of Cistinexine Hydrochloride[J].Fine Chemical Intermediates,2010,40(3):34-36.
Authors:ZHAO Ming-ming  LI Ying  LI Yan-song  SONG Hong-rui
Affiliation:(School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang 110016, China)
Abstract:Cistinexine(5) was synthesized in overall yield of 40% from L-cystine through protection of amino group with benzyl chloroformate ,chlorination with PC15 and reaction with bromohexine. The title compound was obtained from 5 in ethanol-HC1 solution. The structure of eistinexine was confirmed with LC-MS, IR and 1H NMR.
Keywords:cistinexine hydrochloride  medicinal chemistry  process improvement  expectorant drug
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