CAS: 142217-77-4; (1S,2S,3S,5S)-5-(2-Amino-6-(Benzyloxy)-9H-Purin-9-yl)-3-(Benzyloxy)-2-(Benzyloxymethyl)Cyclopentanol

相似化合物

142217-78-5 1907700-40-6 204845-95-4

上下游产品

O-6-苄基鸟嘌呤 2-Amino-6-Benzyloxypurine 19916-73-5

(1S-反式)-2-[(苯甲氧基)甲基]-3-环戊烯-1-醇置于叔丁基过氧化氢,Sodium Hydride,Bis(Acetylacetonato) Oxovanadium(Iv),Lithium Hydroxide体系中,用 四氢呋喃,二氯甲烷,N,N-二甲基甲酰胺 用作溶剂,化学反应 0.17H,反应生成(1S,2S,3S,5S)-5-(2-氨基-6-苄氧基-9H-嘌呤-9-基)-3-苄氧基-2-苄氧基甲基环戊醇
参考文献:恩替卡韦中间体制备新工艺方法及分析方法
标题:恩替卡韦中间体制备新工艺方法及分析方法
摘要:本发明属于化合物技术领域,公开了一种恩替卡韦中间体制备新工艺方法,环戊二烯钠与苄基氯甲基醚反应,再滴加三氟化硼‑thf络合物,氧化水解,淬灭,脱溶,得到中间体s01;将中间体s01在催化剂下经叔丁基过氧化氢氧化,淬灭,水洗脱溶,得到中间体s02;将中间体s02,氢化钠反应,再滴加溴化苄反应,反应完全后加乙醇淬灭反应,减压脱溶用乙酸乙酯/水萃取分液,有机相脱溶后得到中间体s03;S03与o‑6‑苄基鸟嘌呤在催化剂下于有机溶剂中搅拌反应完全,减压脱去dmf,剩余物经硅胶层析提纯,再重结晶得到成品.采用全新的工艺,替换手性硼试剂,消除隐患;同时采用全新的提纯方法,避免产生大量固体废弃物,同时节约时间成本,降低工时,利于工业化生产.

专利信息

专利号:US-2011245484-A1
优先权日:2010-03-31
标 题 :Stereoselective synthesis of phosphorus containing actives

专利号:EP-2752422-A1
优先权日:2010-03-31
标 题 :Stereoselective synthesis of phosphorus containing actives

专利号:EP-2752422-B1
优先权日:2010-03-31
标题:Stereoselective synthesis of phosphorus containing actives

专利号:EP-2552931-B1
优先权日:2010-03-31
标题:Stereoselective synthesis of phosphorus containing actives

专利号:US-8859756-B2
优先权日:2010-03-31
标 题 :Stereoselective synthesis of phosphorus containing actives
发明人：ROSS BRUCE S; SOFIA MICHAEL JOSEPH; PAMULAPATI GANAPATI REDDY; RACHAKONDA SUGUNA; ZHANG HAI-REN
权利人:ROSS BRUCE S; SOFIA MICHAEL JOSEPH; PAMULAPATI GANAPATI REDDY; RACHAKONDA SUGUNA; ZHANG HAI-REN; GILEAD PHARMASSET LLC
摘要:Disclosed herein are phosphorus-containing actives, their use as actives for treating diseases, and a stereoselective process for preparing the same. Also disclosed herein are useful synthetic intermediates and processes for preparing the same.