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Studies on Synthesis and Intramolecular Catalyzed Hydrolysis of Thiophosphoramidate Derivatives of Nucleoside
作者姓名:苗志伟  付华  冯玉萍  韩波  涂光忠  赵玉芬
作者单位:MIAO,Zhi-Wei a FU,Hua a FENG,Yu-Ping a HAN,Bo a TU,Guang-Zhong b ZHAO,Yu-Fen,a a Key Laboratory of Bioorganic Phosphorus Chemistry,Ministry of Education,Department of Chemistry,School of Life Sciences and Engineering
基金项目:theNationalNaturalScienceFoundationofChina (Nos .2 990 2 0 0 3and 39870 415 ) ,theMinistryofScienceandTechnology ,theEducationMinistryofChinaandDoctorCandidateInnovationFoundationinTsinghuaUniversity (No .0 92 430 30 5 )
摘    要:IntroductionNucleosidesandtheiranaloguesaspotentialanti cancerandantivirusagentshavebeenstudiedextensively .Mostofthecurrentlylicensedantiviraldrugsandmanyofthedrugsusedinanticancerchemotherapyarenucleosideanalogues .1Forthemajorityoftheseanaloguesshown…


Studies on Synthesis and Intramolecular Catalyzed Hydrolysis of Thiophosphoramidate Derivatives of Nucleoside
MIAO,Zhi-Wei a FU,Hua a FENG,Yu-Ping a HAN,Bo a TU,Guang-Zhong b ZHAO,Yu-Fen,a a Key Laboratory of Bioorganic Phosphorus Chemistry,Ministry of Education.Studies on Synthesis and Intramolecular Catalyzed Hydrolysis of Thiophosphoramidate Derivatives of Nucleoside[J].Chinese Journal of Chemistry,2002,20(11):1434-1438.
Authors:MIAO  Zhi-Wei a FU  Hua a FENG  Yu-Ping a HAN  Bo a TU  Guang-Zhong b ZHAO  Yu-Fen  a a Key Laboratory of Bioorganic Phosphorus Chemistry  Ministry of Education
Institution:MIAO,Zhi-Wei a FU,Hua a FENG,Yu-Ping a HAN,Bo a TU,Guang-Zhong b ZHAO,Yu-Fen,a a Key Laboratory of Bioorganic Phosphorus Chemistry,Ministry of Education,Department of Chemistry,School of Life Sciences and Engineering
Abstract:Novel thiophosphoramidate derivatives of nucleoside analogue as membrane‐soluble prodrugs of the bioactive free nucleotides have been prepared by thiophosphorylation reaction. 2′,3′‐O, O′‐Isopropylidene uridine‐5′‐yl N‐thiophosphoryl serine and threonine methyl esters underwent the intramolecular catalyzed hydrolysis reaction.
Keywords:synthesis  thiophosphoramidate  nucleoside analogue  hydrolysis reaction  mechanism
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