| 標題: | Convenient Synthesis of AZT/d4t Phosphoramidate or Aryl Phosphate Monoesters by Mg-Cleavage 4-Picolyl Protected Group |
| 作者: | An-Fu Hu
Zhen-Yu Zheng
Neng-Ming Jin
Peng-Xiang Xu
Yu-Fen Zhao |
| 貢獻者: | Department of Chemistry and The Key Laboratory for Chemical Bilolgy of Fujian Province, College of Chemistry and Chemical Engineering |
| 關鍵字: | Nucleoside derivatives pro-drug
4-picolyl
Mg
deprotection method |
| 日期: | 2008-07 |
| 上傳時間: | 2017-12-04 15:57:32 (UTC+8) |
| 摘要: | The development of nucleoside pro-drugs capable of umdergoing intracellular activation to the corresponding nucleotides has become an area of intense interest. Nucleoside phosphoramidate to the monoesters are potent antiviral and/or anticancer agents with enhanced activity and reduced cytotoxicity. Likewise, nucleoside aryl phosphate monoesters can serve as ready pro-drug sources of free nucleosides and their 5’-monophosphates. In this work, we report a simple approach to stynthesize AZT/d4T phoshoramidate or aryl phosphate monoesters by Mg-cleavage 4-picolyl protected group. A typical process is depicted below. |
| 關聯: | 第五屆海峽化學、生物及材料研討會，起迄日：2008/07/21-2008/07/22，地點：嘉南藥理科技大學 |
| 显示于类别: | [藥理學院] 2008第五屆海峽化學、生物及材料研討會
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