CAS: 143491-57-0; 4-Amino-5-Fluoro-1-((2R,5S)-2-(Hydroxymethyl)-1,3-Oxathiolan-5-yl)Pyrimidin-2(1H)-One

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(1R,2S,5R)-2-Isopropyl-5-Methylcyclohexyl (2R,5S)-5-[5-Fluoro-2-Oxo-4-(Phenylcarboxamido)-1,2-Dihydro-1-Pyrimidinyl]-1,3-Oxathiolane-2-Carboxylate置于甲醇,Sodium Tetrahydroborate,Dipotassium Hydrogenphosphate,水,Sodium Hydroxide体系中,用 甲醇 用作溶剂,化学反应 1.0H,以75%的收率获得恩曲他滨
参考文献:Highly Stereoselective Synthesis Of Lamivudine (3Tc) And Emtricitabine (Ftc) By A Novel N-Glycosidation Procedure
标题:Highly Stereoselective Synthesis Of Lamivudine (3Tc) And Emtricitabine (Ftc) By A Novel N-Glycosidation Procedure
摘要:The Combined Use Of Silanes (Et3Sih Or Pmhs) And I-2 As Novel N-Glycosidation Reagents For The Synthesis Of Bioactive Oxathiolane Nucleosides 3Tc And Ftc Is Reported. Both Systems (Working As Anhydrous Hi Sources) Were Devised To Act As Substrate Activators And N-Glycosidation Promoters. Excellent Results In Terms Of Chemical Efficiency And Stereoselectivity Of The Reactions Were Obtained; Surprisingly,The Nature Of The Protective Group At The N4 Position Of (Fluoro)Cytosine Additionally Influenced The Stereochemical Reaction Outcome.
Doi:10.1021/acs.Orglett.5B00982