863329-65-1 = 863329-66-2 反应条件:1.1 Reagents: Ammonia Solvents: Methanol; 8 - 12 H,Rt 标题:Design,Synthesis,And Antiviral Activity Of 2'-Deoxy-2'-Fluoro-2'-C-Methyl-Cytidine,A Potent Inhibitor Of Hepatitis C Virus Replication 作者:Clark,Jeremy L.; Et Al 参考文献:Journal Of Medicinal Chemistry 日期:2005 卷标:48(17) 页码:5504-5508]
817204-32-3 = 863329-66-2 反应条件:1.1 Reagents: Acetic Acid Solvents: Water; 20 H,Rt -> 110 °C1.2 Reagents: Ammonia Solvents: Methanol; 3 H,0 °C; 24 H,0 °C -> 15 °C 标题:Discovery Of A β-D-2'-Deoxy-2'-α-Fluoro-2'-β-C-Methyluridine Nucleotide Prodrug (Psi-7977) For The Treatment Of Hepatitis C Virus 作者:Sofia,Michael J.; Et Al 参考文献:Journal Of Medicinal Chemistry 日期:2010 卷标:53(19) 页码:7202-7218
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:US-2018162896-A1 优先权日:2015-05-26 标题 :Synthesis of Phosphoramidates 发明人:WILHELM THORSTEN; SCHÖNE OLGA; SPITZENSTÄTTER HANS-PETER 权利人:SANDOZ AG 摘要:A process for preparing a nucleoside phosphoramidate, in particular to a process for preparing sofosbuvir, wherein a phosphoramidate derivative is used as starting material.
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
专利号:CA-2954940-A1 优先权日:2014-07-31 标 题 :Synthesis of phosphoramidates
1: Lawitz E, Rodriguez-Torres M, Denning JM, Albanis E, Cornpropst M, Berrey MM, Symonds WT. Pharmacokinetics, pharmacodynamics, and tolerability of GS-9851, a nucleotide analog polymerase inhibitor, following multiple ascending doses in patients with chronic hepatitis C infection. Antimicrob Agents Chemother. 2013 Mar;57(3):1209-17. doi: 10.1128/AAC.01263-12. Epub 2012 Dec 21. 2: Denning J, Cornpropst M, Flach SD, Berrey MM, Symonds WT. Pharmacokinetics, safety, and tolerability of GS-9851, a nucleotide analog polymerase inhibitor for hepatitis C virus, following single ascending doses in healthy subjects. Antimicrob Agents Chemother. 2013 Mar;57(3):1201-8. doi: 10.1128/AAC.01262-12. Epub 2012 Dec 21. 3: Murakami E, Niu C, Bao H, Micolochick Steuer HM, Whitaker T, Nachman T, Sofia MA, Wang P, Otto MJ, Furman PA. The mechanism of action of beta-D-2'-deoxy-2'-fluoro-2'-C-methylcytidine involves a second metabolic pathway leading to beta-D-2'-deoxy-2'-fluoro-2'-C-methyluridine 5'-triphosphate, a potent inhibitor of the hepatitis C virus RNA-dependent RNA polymerase. Antimicrob Agents Chemother. 2008 Feb;52(2):458-64. Epub 2007 Nov 12.