抗肿瘤药物达卡巴嗪合成工艺的优化

中国药物化学杂志 Pub Date : 2015-01-01 DOI:10.6023/CJOC201410026

Shengwei Xiao, Zhijun Liu, Yang Liu, Heru Chen

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引用次数: 0

摘要

以甘氨酸为原料，经酯化、甲酰化、脱水、酰胺化4步反应制得2-异氰乙酰胺，总收率为42.9%。2异氰乙酰胺与氰酰胺在碱性条件下进行环化反应，得到重要中间体5-氨基- 1h -咪唑-4-羧酰胺，收率为68.2%。该中间体经过重氮化，随后与二甲胺偶联反应得到目标化合物。总收益率为22.3%。所有中间体和目标产物达卡巴嗪经核磁共振氢谱、核磁共振碳谱和质谱确证。该工艺具有材料便宜、条件温和、总收率高的经济效益。

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Optimization of the Synthetic Process of Antineoplastic Drug Dacarbazine

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%. 2Isocyanoacetamide 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 H NMR, C NMR and ESI-MS. The current process is economic efficient characterized by applied cheap materials, mild conditions, and good overall yield.

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来源期刊

中国药物化学杂志

自引率

0.00%

发文量

3349

期刊介绍： The Chinese Journal of Medicinal Chemistry is jointly sponsored by Shenyang Pharmaceutical University and the Chinese Pharmaceutical Society. It is the only professional academic journal in China that specifically reflects the scientific research results and scientific and technological information in the field of medicinal chemistry. Its purpose is to stand at the forefront of the development of medicinal chemistry today, report the latest scientific and technological trends and scientific research results of the discipline, provide a window for the vast number of medical and scientific workers to understand new drug research, pharmaceutical process research, and natural drug chemistry research, and promote the development of the world's pharmaceutical industry. The readers are researchers in the fields of pharmacy, chemistry, biology, and traditional Chinese medicine in drug research institutes, research institutes, and pharmaceutical companies; teachers, scientific researchers, and graduate students in domestic and foreign medical schools; scientific and technological management cadres and medical intelligence personnel related to pharmacy and pharmaceuticals, etc.