CAS: 229614-55-5; Peramivir

上下游产品

14H25N2O4(1-)*Na(1+)C14H25N2O4(1-)*Na(1+) 2-Ethylbutyraldehyde (-)-(1S,2S,3R,4R)-3-[(1S)-1-(Acetylamino)-2-ethylbutyl]-4-({[(tert-butoxycarbonyl)amino][(tert-butoxycarbonyl)-imino]methyl}amino)-2-hydroxycyclopentanecarboxylic Acid (1S,4R)-methyl-4-(2,3-bis(tert-butoxycarbonyl)guanidino)cyclopent-2-ene-carboxylate

(1S,4R)-4-甲基环戊-2-烯甲酸甲酯盐酸盐置于盐酸,Sodium Hypochlorite,Sodium Tetrahydroborate,Nickel(II) Chloride Hexahydrate,Sodium Carbonate,三乙胺,Sodium Hydroxide体系中,用 甲醇,乙醚,正己烷,二氯甲烷,水,N,N-二甲基甲酰胺 用作溶剂,化学反应 94.5H,反应生成帕拉米韦三水
参考文献:Facile Synthesis Of The Neuraminidase Inhibitor Peramivir
标题:Facile Synthesis Of The Neuraminidase Inhibitor Peramivir
摘要:An Improved And Convenient Synthetic Route For The Synthesis Of Peramivir Has Been Developed With A Total 34% Yield. The Process Was Improved From Previous Methods In Three Key Reaction Steps Including 1,3-Dipolar Cycloaddition,Reductive Ring Cleavage Of The Isoxazoline,And Incorporation Of The Peripheral Guanidino Group. First,An Activated Sodium Hypochlorite (Cl%=10%) Was Employed For The Catalytic 1,3-Dipolar Cycloaddition,And 61-68% Yields Were Obtained. Second,The Nabh4-Nicl2 Was Used As A New Reducing Reagent Instead Of The Expensive Catalyst Pto2. Most Important,An Innovative And Environmentally Friendly Method Of Guanylation In The Final Step Was Developed Using Chloroformamidine Hydrochloride As The Amidino Reagent,Which Avoided The Use Of The Highlytoxic Reagent Of Hgcl2 And Made The Process Greener. Supplemental Materials Are Available For This Article. Go To The Publisher'S Online Edition Of Synthetic Communications (R) To View The Free Supplemental File.
Doi:10.1080/00397911.2012.729279