Chin. J. Org. Chem. ›› 2015, Vol. 35 ›› Issue (5): 1161-1165.DOI: 10.6023/cjoc201410026 Previous Articles     Next Articles



肖胜伟a, 刘志军a, 柳杨a, 陈河如a,b   

  1. a 暨南大学药学院中药及天然药物研究所 广州 510632;
    b 广东省中药药效物质基础及创新药物研究重点实验室 广州 510632
  • 收稿日期:2014-10-18 修回日期:2014-12-19 发布日期:2015-01-07
  • 通讯作者: 陈河如
  • 基金资助:


Optimization of the Synthetic Process of Antineoplastic Drug Dacarbazine

Xiao Shengweia, Liu Zhijuna, Liu Yanga, Chen Herua,b   

  1. a Institute of Traditional Chinese Medicine and Natural Products, College of Pharmacy, Jinan University, Guangzhou 510632;
    b Guangdong Province Key Laboratory of Pharmacodynamic Constituents of TCM and New Drugs Research, Jinan University, Guangzhou 510632
  • Received:2014-10-18 Revised:2014-12-19 Published:2015-01-07
  • Supported by:

    Project supported by the National Natural Science Foundation of China (No.81172982).

Dacarbazine has been prepared started from glycine, which was carried on firstly through a four-step process including esterification, formylation, dehydration, amidation to give 2-isocyanoacetamide with a total yield of 42.9%. 2-Isocyanoacetamide was then cyclized with cyanamide under basic condition to afford the important intermediate 5-amino-1H-imidazole-4-carboxamide with yield of 68.2%. This intermediate undergoing diazotization and following coupling reaction with dimethylamine led to the target compound. The overall yield was 22.3%. All the intermediates and the target products dacarbazine were confirmed by 1H NMR, 13C NMR and ESI-MS. The current process is economic efficient charac-terized by applied cheap materials, mild conditions, and good overall yield.

Key words: dacarbazine, process optimization, drug synthesis, anticancer