CAS: 1244022-55-6; ((Hydroxy((((R)-1-(6-((Hydroxymethyl)Amino)-9H-Purin-9-yl)Propan-2-yl)Oxy)Methyl)Phosphoryl)Oxy)Methyl Isopropyl Carbonate

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chloromethyl isopropyl carbonate tenofovir adenine (R)-9-(2-hydroxypropyl)adenine

📜腺嘌呤置于三甲基氯硅烷,Magnesium 2-Methylpropan-2-Olate,三乙胺,Sodium Bromide,Sodium Hydroxide体系中,用 N-甲基吡咯烷酮,N,N-二甲基甲酰胺 用作溶剂,化学反应 5.5H,反应生成替诺福韦杂质w,6N-羟甲基替诺福韦二吡呋酯
参考文献:Process Improvements For The Manufacture Of Tenofovir Disoproxil Fumarate At Commercial Scale
标题:Process Improvements For The Manufacture Of Tenofovir Disoproxil Fumarate At Commercial Scale
摘要:The Three-Step Manufacturing Process Used In The Synthesis Of Tenofovir Disoproxil Fumarate (1) Was Studied And Optimized,Leading To A More Productive And Robust Process. The Yield Was Improved From About 13% Overall To 24%. Key Process Improvements Identified Included Implementation Of A Telescoped Process For The Second Stage That Obviated The Need For An Extraction And Solvent Exchange,And Significant Optimization Of The Final Reaction,Including The Beneficial Effect Of Adding A Quaternary Ammonium Salt To The Alkylation Reaction And Development Of A Nonaqueous Process For Removal Of Nmp And Triethylamine From The Product Mixture To Decrease The Level Of Decomposition Of Product During The Isolation.
Doi:10.1021/op1001337