专利号:US-10995093-B2 优先权日:2016-04-07 标 题 :Synthesis of 2′-fluoro-6′-methylene-carbocyclic adenosine (FMCA) and 2′-fluoro-6′methylene-carbocyclic guanosine (FMCG) 发明人:CHU CHUNG K; MULAMOOTTTIL VARUGHESE ALEXANDER; MISHRA RAM C; SINGH UMA SHARAN 权利人:UNIV GEORGIA 摘要:The invention provides a new convergent approach for the synthesis of 2′-fluoro-6′-methylene-carbocyclic adenosine (FMCA) and 2′-fluoro-6′-methylene-carbocyclic guanosine (FMCG) from a readily available starting material in eight steps. An efficient and practical methodology for stereospecific preparation of a versatile carbocyclic key intermediate, (1S,3R, 4R)-3-tert-butoxy-4-(tert-butoxymethyl)-2-fluoro-5-methylenecyclopentanol (compound 8 of scheme 1A or a) in only six (6) steps is also provided. Prodrugs of these compounds are also prepared.
专利号:US-2017218006-A1 优先权日:2014-07-31 标题 :Synthesis of Phosphoramidates 发明人:WILHELM THORSTEN; SPITZENSTÄTTER HANS-PETER; SCHÖNE OLGA; RICHTER FRANK; SCHREINER ERWIN 权利人:SANDOZ AG 摘要:A process for the preparation of a compound of formula (I) including all isomers, stereoisomers, enantiomers and diastereomers thereof (I), and salts thereof; the process comprising providing a mixture comprising a compound of formula (II) and a compound of formula (III) subjecting the mixture provided in a) to reaction conditions in the presence of one or more Lewis acids to the mixture provided in a), obtaining a mixture comprising the compound of formula (I).
专利号:WO-2021083438-A1 优先权日:2019-10-30 标 题:Inhibitors of purine nucleoside phosphorylase - synthesis and use thereof for treatment of t-cell acute lymphoblastic leukemia and lymphoma 发明人:SKACEL JAN; JANEBA ZLATKO; MERTLIKOVA KAISEROVA HELENA 权利人:USTAV ORGANICKE CHEMIE A BIOCHEMIE AV CR V V I 摘要:The present invention relates to new compounds of general formula I, their synthesis, their pharmaceutically acceptable salts, and their use in treatment of T-cell acute lymphoblastic leukemia and lymphoma.
专利号:EP-3174892-A1 优先权日:2014-07-31 标 题:Synthesis of phosphoramidates
专利号:US-2014309413-A1 优先权日:2013-03-11 标题 :Methods of stereoselective synthesis of substituted nucleoside analogs 发明人:ROSE PETER JAMISON; JUNG YOUNG CHUN; BLIGH CAVAN MCKEON; IBRAHIM SHEREEN; ANZALONE LUIGI; MILLER JR DAVID B; VAN ALSTEN JOHN GREGG; CURRAN TIMOTHY THOMAS 权利人:VERTEX PHARMA 摘要:The present invention relates to the novel diastereoselective syntheses for generating phosphorothioate compounds. Examples include nucleoside phosphorothioate analogs that are useful in treating diseases and/or conditions such as viral infections.
专利号:US-2011245484-A1 优先权日:2010-03-31 标 题 :Stereoselective synthesis of phosphorus containing actives