A practical synthesis of trifluorophenyl R-amino acid: The key precursor for the new anti-diabetic drug sitagliptin
文献类型：期刊论文
| 作者 | Zeng Li Li2; Ding Ying Jie2; Zhang Gui Cheng2; Song Hong Rui1; Hu Wen Hui2 |
| 刊名 | CHINESE CHEMICAL LETTERS
 |
| 出版日期 | 2009 |
| 卷号 | 20期号:12页码:1397-1399 |
| 关键词 | PEPTIDASE-IV INHIBITORS GENERATION POTENT Sitagliptin beta-Amino acid DPP-IV inhibitor Practical synthesis |
| ISSN号 | 1001-8417 |
| 英文摘要 | Sitagliptin is the first new anti-diabetic drug in DPP-IV inhibitor class. The general synthesis of sitagliptin is by coupling of the beta-amino acid fragment with the heterocycle fragment. Though the specific beta-amino acid can be easily made from the corresponding R-amino acid by Arndt-Eistert homologation, the optically pure precursor R-amino acid is difficult to prepare. We herein reported a practical protocol to make the trifluorophenyl substituted R-amino acid 4 in >99.9% ee and 40.3% yield by the enzymatic resolution employing enantioselective hydrolysis and a general separation procedure. This protocol requires only cheap starting materials and friendly reaction condition. The procedure not only allows people to prepare the drug substance, but also provides an alternative method for prepareing the rare a-amino acid and the subsequent beta-amino acid. (C) 2009 Wen Hui Hu. Published by Elsevier B.V. on behalf of Chinese Chemical Society. All rights reserved. |
| 资助项目 | [Guangdong Province] |
| 语种 | 英语 |
| CSCD记录号 | CSCD:3778155 |
| 源URL | [http://ir.imr.ac.cn/handle/321006/156572]  |
| 专题 | 金属研究所_中国科学院金属研究所 |
| 作者单位 | 1.中国科学院金属研究所 2.中国科学院 |
| 推荐引用方式 GB/T 7714 | Zeng Li Li,Ding Ying Jie,Zhang Gui Cheng,et al. A practical synthesis of trifluorophenyl R-amino acid: The key precursor for the new anti-diabetic drug sitagliptin[J]. CHINESE CHEMICAL LETTERS,2009,20(12):1397-1399. |
| APA | Zeng Li Li,Ding Ying Jie,Zhang Gui Cheng,Song Hong Rui,&Hu Wen Hui.(2009).A practical synthesis of trifluorophenyl R-amino acid: The key precursor for the new anti-diabetic drug sitagliptin.CHINESE CHEMICAL LETTERS,20(12),1397-1399. |
| MLA | Zeng Li Li,et al."A practical synthesis of trifluorophenyl R-amino acid: The key precursor for the new anti-diabetic drug sitagliptin".CHINESE CHEMICAL LETTERS 20.12(2009):1397-1399. |
入库方式： OAI收割
来源：金属研究所
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