| 谭新刚,施小新,孟天卓,章强,郑波.化学通报,2016,79(12):1189-1191. |
| 生物素手性中间体的合成 |
| Preparation of the Chiral Intermediate for ( )-Biotin Synthesis |
| 投稿时间：2015-08-04 修订日期：2016-06-28 |
| DOI： |
| 中文关键词: 乙内酰脲 L-半胱氨酸 苯甲醛 一锅法 合成 |
| 英文关键词:Hydantoin L-cysteine benzaldehyde one-pot synthesis |
| 基金项目:国家自然科学基金资助项目(20972048)；上海市教育发展基金资助项目(03SG27) |
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| 中文摘要: |
| 以L-半胱氨酸与苯甲醛为起始原料,缩合生成(4R)-2-苯基四氢噻唑-4-羧酸(2),甲酯化制得(4R)-2-苯基四氢噻唑-4-甲酸甲酯(3),然后与三光气、苄胺经“一锅法”合成乙内酰脲(1),三步反应总收率87%,其结构经1H NMR,13C NMR,IR和MS表征。此法绿色环保、成本较低,适合工业化生产。 |
| 英文摘要: |
| (4R)-2-Phenylthiazolidine-4-carboxylic acid (2) was prepared from L-cysteine and benzaldehyde. Esterification of compound 2 produced (4R)-methyl-2-phenylthiazolidine-4-carboxylate. Then hydantoin (1) was obtained via a one-pot reaction of compound 3 with triphosgene and benzylamine. The total yield of the three steps is approximately 87%. The structures of compounds 1-3 were characterized by 1H NMR, 13C NMR,IR and MS. The method is environmentally friendly, lower cost, and suitable for industrial production. |
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