甲基苯醌置于potassium Hydride,臭氧,三苯基膦体系中,化学反应 13.5H,反应生成 苄氧基乙醛 参考文献:A Route To The Pyrrolo[1,2-A]Indolenine Ring System Via Intermolecular Organolithium Addition To An Oxindole 标题:A Route To The Pyrrolo[1,2-A]Indolenine Ring System Via Intermolecular Organolithium Addition To An Oxindole 摘要:A Synthesis Of The Pyrrolo[1,2 A]Indolenine 6 In Four Steps From N-Benzyl-3,3-Dimethyloxindole 2 Is Presented Involving An Organolithium Addition To The Oxindole Carbonyl Group. Additions Of Vinyllithiums To The Oxindole 2 Are Presented. DOI:10.1016/s0040-4020(01)80407-5
专利号:US-6069250-A 优先权日:1995-12-14 标 题 :Method and compositions for the synthesis of dioxolane nucleosides with β-configuration 发明人:MANSOUR TAREK; CIMPOIA ALEX; BEDNARSKI KRZYSZTOF 权利人:IAF BIOCHEM INT 摘要:The present invention relates to methods and compositions for preparing biologically important nucleoside analogues containing 1,3-dioxolane sugar rings. In particular, this invention relates to the stereoselective synthesis of the beta (cis) isomer by glycosylating the base with an intermediate of formula (II) below a temperature of about -10 DEG C. wherein R1 and L are as defined herein.
专利号:EP-2465936-A1 优先权日:2010-12-20 标题 :Enzymatic synthesis of statins and intermediates thereof 权利人:LEK PHARMACEUTICALS 摘要:The present invention discloses a process for preparing an active pharmaceutical ingredient (API) or intermediates thereof, notably particular step in the synthesis of an intermdiate useful for example in the preparation of statins, by using an enzyme capable of catalyzing oxidation or dehydrogenation. The invention further provides an expression system effectively translating said enzyme. In addition, the invention relates to a specific use of such enzyme for preparing API or intermediate thereof, and in particular for preparing statin or interemediate thereof.
专利号:US-7541456-B2 优先权日:2002-04-19 标题:Direct, enantioselective aldol coupling of aldehydes using chiral organic catalysts 发明人:MACMILLAN DAVID W C; NORTHRUP ALAN B 权利人:CALIFORNIA INST OF TECHN 摘要:Nonmetallic, chiral organic catalysts are used to catalyze an enantioselective aldol coupling reaction between aldehyde substrates. The reaction may be carried out with a single enolizable aldehyde, resulting in dimerization to give a β-hydroxy aldehyde, or trimerization to give a dihydroxy tetrahydropyran. The reaction may also conducted with an enolizable aldehyde and a second aldehyde, which may or may not be enolizable, so that the coupling is a cross-aldol reaction in which the α-carbon of the enolizable aldehyde adds to the carbonyl carbon of the second aldehyde in an enantioselective fashion. Reaction systems composed of at least one enolizable aldehyde, an optional additional aldehyde, and the nonmetallic chiral organic catalyst are also provided, as are methods of implementing the enantioselective aldol reaction in the synthesis of sugars.
专利号:WO-9946267-A1 优先权日:1998-03-12 标题 :Modulators of protein tyrosine phosphatases (ptpases) 发明人:MOELLER NIELS PETER HUNDAHL; ANDERSEN HENRIK SUNE; IVERSEN LARS FOGH; OLSEN OLE HVILSTED; BRANNER SVEN; HOLSWORTH DANIEL DALE; BAKIR FARID; JUDGE LUKE MILBURN; AXE FRANK URBAN; JONES TODD KEVIN; RIPKA WILIAM CHARLES; GE YU; UYEDA ROY TERUYUKI 权利人:NOVO NORDISK AS; ONTOGEN CORP 摘要:The present invention provides novel compounds, novel compositions, methods of their use, and methods of their manufacture, where such compounds are pharmacologically useful inhibitors of Protein Tyrosine Phosphatases (PTPases) such as PTP1B, CD45, SHP-1, SHP-2, PTPα, LAR and HePTP or the like. The compounds are useful in the treatment of type I diabetes, type II diabetes, impaired glucose tolerance, insulin resistance, obesity, immune dysfunctions including autoimmunity diseases with dysfunctions of the coagulation system, allergic diseases including asthma, osteoporosis, proliferative disorders including cancer and psoriasis, diseases with decreased or increased synthesis or effects of growth hormone, diseases with decreased or increased synthesis of hormones or cytokines that regulate the release of/or response to growth hormone, diseases of the brain including Alzheimer's disease and schizophrenia, and infectious diseases.
专利号:US-6951878-B2 优先权日:1998-03-12 标 题:Benzo[b]thiophenyl or tetrahydro-benzo[b]thiophenyl modulators of protein tyrosine phosphatases (PTPases) 发明人:MOELLER NIELS PETER HUNDAHL; ANDERSEN HENRIK SUNE; IVERSEN LARS FOGH; OLSEN OLE HVILSTED; BRANNER SVEN; HOLSWORTH DANIEL DALE; BAKIR FARID; JUDGE LUKE MILBURN; AXE FRANK URBAN; JONES TODD KEVIN; RIPKA WILLIAM CHARLES; GE YU; UYEDA ROY TERUYUKI 权利人:NOVO NORDISK AS 摘要:The present invention provides novel compounds, novel compositions, methods of their use, and methods of their manufacture, where such compounds are pharmacologically useful inhibitors of Protein Tyrosine Phosphatases (PTPase's) such as PTP1B, CD45, SHP-1, SHP-2, PTPα, LAR and HePTP or the like. n The compounds are useful in the treatment of type I diabetes, type II diabetes, impaired glucose tolerance, insulin resistance, obesity, immune dysfunctions including autoimmunity diseases with dysfunctions of the coagulation system, allergic diseases including asthma, osteoporosis, proliferative disorders including cancer and psoriasis, diseases with decreased or increased synthesis or effects of growth hormone, diseases with decreased or increased synthesis of hormones or cytokines that regulate the release of/or response to growth hormone, diseases of the brain including Alzheimer's disease and schizophrenia, and infectious diseases.
专利号:US-9243002-B2 优先权日:2013-02-07 标题 :Tetracyclic heterocycle compounds and methods of use thereof for the treatment of hepatitis C 发明人:DAI XING; LIU HONG; PALANI ANANDAN; HE SHUWEN; BROCKUNIER LINDA L; NARGUND RAVI; MARCANTONIO KAREN; ZORN NICOLAS; XIAO DONG; PENG XUANJIA; LI PENG; GUO TAO 权利人:MERCK SHARP & DOHME 摘要:The present invention relates to compounds of formula I that are useful as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.
参考标题:Total Synthesis Of The Macrolide Antibiotic Cytovaricin 作者:David A. Evans,Stephen W. Kaldor,Todd K. Jones,Jon Clardy,Thomas J. Stout |发布日期:1990.9 摘要:A Convergent Asymmetric Synthesis Of The Antinoeplastic Macrolide Antibiotic Cytovaricin Has Been Achieved Through The Synthesis And Coupling Of The Illustrated Spiroketal And Polyol Glycoside Subunits. All Absolute Steroechemical Relationships Within The Target Structure Were Ultimately Controlled By The Use Of Asymmetric Aldol, Alkylation, Or Epoxidation Methodology. Union Of The Two Subnits Was
合成参考文献
摘要:Li, W.; Liu, X. H.; Feng, X. M., Science of Synthesis Knowledge Updates, (2021) 1, 48. 摘要:Wu, X.-F., Science of Synthesis Knowledge Updates, (2014) 1, 255. 摘要:Matsunaga, S., Science of Synthesis Knowledge Updates, (2010) 4, 209. 摘要:Snaith, J. S., Science of Synthesis Knowledge Updates, (2011) 2, 250. 摘要:Khartulyari, A.; Maier, M. E., Science of Synthesis Knowledge Updates, (2010) 3, 100.