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抗肿瘤药奥沙利铂的合成工艺改进
引用本文:王庆琨,普绍平,彭 娟,刘凉萌,廖云星,晋 杰. 抗肿瘤药奥沙利铂的合成工艺改进[J]. 中国药物化学杂志, 2013, 23(2): 106-107,126
作者姓名:王庆琨  普绍平  彭 娟  刘凉萌  廖云星  晋 杰
作者单位:(昆明贵研药业有限公司 云南省铂族金属抗肿瘤药物工程技术研究中心,云南 昆明 650106)
基金项目:国家科技型中小企业技术创新基金项目(11C26215305898);云南省重点科技计划项目(2010DH021)
摘    要:
目的合成抗肿瘤药物奥沙利铂。方法以氯亚铂酸钾为起始原料,先后与亚硝酸钠、(1R,2R)-环己二胺、硫酸肼、一水合草酸钾反应合成目标化合物。合成的化合物采用元素分析、质谱、红外光谱、核磁共振氢谱和比旋光度对其结构进行表征。结果与结论合成的化合物结构与标题化合物一致,精品收率为52%。本方法为奥沙利铂的合成提供了一条新型的工艺路线。

关 键 词:铂配合物  奥沙利铂  合成
收稿时间:2012-09-06
修稿时间:2013-02-25

Improved synthesis of antitumor drug oxaliplatin
WANG Qing-kun,PU Shao-ping,PENG Juan,LIU Liang-meng,LIAO Yun-xing,JIN Jie. Improved synthesis of antitumor drug oxaliplatin[J]. Chinese Journal of Medicinal Chemistry, 2013, 23(2): 106-107,126
Authors:WANG Qing-kun  PU Shao-ping  PENG Juan  LIU Liang-meng  LIAO Yun-xing  JIN Jie
Affiliation:(Yunnan Engineering and Technology Center of Platinum-based Anti-tumor Drug, Kunming Gui Yan Pharmaceutical Co., Ltd., Kunming 650106, China)
Abstract:
The preparation of platinum-based antitumor drug oxaliplatin was achieved via a four-step sequence from K4PtCl4. K4PtCl4 was treated with sodiunmitrite to give the K4Pt( NO2 )4 solution, then which was reacted with( 1R ,2R) -1,2-cyclohexanediamine to give the key intermediate Pt( C6H14N2 ) ( NO2 ) 2. The key intermediate was subsequently reacted with hydrazine sulfate and potassium oxalate monohydrate to give target compound. The structure of the target compound was identified by elemental analysis, ESI-MS, FT-IR, 1H-NMR and specific rotatory power. The result showed that its structure was consistent with the title compound,the yield was about 52%. This article provides a novel process for the praparation of oxaliplatin.
Keywords:platinum complex  oxaliplatin  synthesis
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