Convenient Synthesis of AZT/d4t Phosphoramidate or Aryl Phosphate Monoesters by Mg-Cleavage 4-Picolyl Protected Group

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Title:	Convenient Synthesis of AZT/d4t Phosphoramidate or Aryl Phosphate Monoesters by Mg-Cleavage 4-Picolyl Protected Group
Authors:	An-Fu Hu Zhen-Yu Zheng Neng-Ming Jin Peng-Xiang Xu Yu-Fen Zhao
Contributors:	Department of Chemistry and The Key Laboratory for Chemical Bilolgy of Fujian Province, College of Chemistry and Chemical Engineering
Keywords:	Nucleoside derivatives pro-drug 4-picolyl Mg deprotection method
Date:	2008-07
Issue Date:	2017-12-04 15:57:32 (UTC+8)
Abstract:	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.
Relation:	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
Appears in Collections:	[Pharmacy and Science] The 5rh Conference of Channel-bridge Chemistry, Biology and materal Science

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