专利号:US-8703952-B2 优先权日:2008-12-12 标题:Synthesis of 9-(arylalkyl)-1,2,3,4-tetrahydro-γ-carboline and analogues and intermediates 发明人:WILLIAMSON CRAIG; STOREY JOHN MERVYN DAVID 权利人:WILLIAMSON CRAIG; STOREY JOHN MERVYN DAVID; WISTA LAB LTD 摘要:The present invention pertains generally to methods of preparing certain 9-(arylalkyl)-1,2,3,4-tetrahydro-γ-carboline compounds and their analogues, and especially to methods of preparing dimebon. The present invention also pertains to methods of preparing certain intermediate compounds which find use in the synthesis of the 9-(arylalkyl)-1,2,3,4-tetrahydro-γ-carboline compounds.
专利号:US-4895996-A 优先权日:1988-10-17 标 题 :Synthesis of alkenes from enamines via hydroboration 发明人:GORALSKI CHRISTIAN T; SINGARAM BAKTHAN; BROWN HERBERT C 权利人:PURDUE RESEARCH FOUNDATION; DOW CHEMICAL CO 摘要:Alkenes are prepared by the hydroboration of enamines followed by an elimination reaction to form the alkene. This process has wide applicability and is useful for the stereospecific synthesis of [Z] isomers. It is preferred to use 9-borabicyclo[3.3.1 nonane as the hydroborating agent and to use methanol to catalyze the elimination reaction.
专利号:US-5461156-A 优先权日:1993-03-31 标 题 :Stereocontrolled synthesis of cis-bicyclic compounds 发明人:KHAU VIEN V; MARTINELLI MICHAEL J; PETERSON BARRY C; SULLIVAN KEVIN A 权利人:LILLY CO ELI 摘要:This invention provides a process for the stereocontrolled synthesis of cis-bicyclic compounds, including cis-hexahydro-6-isoquinolones, cis-dihydroisochromanones, cis-dihydrothiochromanones, and cisbicyclo[4.4.0]dec-3-ene-2-ones.
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-2007129554-A1 优先权日:2005-10-24 标题 :Alpha functionalization of cyclic, ketalized ketones and products therefrom 发明人:HARRINGTON PETER J; KHATRI HIRALAL N; KHATRI SUDHA 权利人:HARRINGTON PETER J; KHATRI HIRALAL N; KHATRI SUDHA 摘要:Methodologies for the alpha-monohalogenation of acid sensitive ketones, especially cyclic, acid-sensitive, ketalized ketones. As one approach, the ketone is reacted with a halogen donor compound, e.g., N-chlorosuccinimide, in anhydrous, highly polar organic reagents such as dimethylformamide (DMF). As another monohalogenation approach, it has been observed that organic salts generated from amines and carboxylic acids catalyze the monohalogenation of ketalized ketone in reagents comprising alcohol solvent (methanol, ethanol, isopropanol, etc.). The monohalogenation is fast even at −5° C. The salt can be rapidly formed in situ from ingredients including amines and/or carboxylic acids without undue degradation of the acid sensitive ketal. Aryl ketones are monooxygenated using iodosylbenzene. This methodology is applied to monohalogenation of an acid sensitive monoketal ketone. The ability to prepare monohalogenated, acid sensitive ketones facilitates syntheses using halogenated, acid sensitive ketones. As just one example, facile synthesis of halogenated, acid sensitive ketones provides a new approach to synthesize the S-ketal-acid S-MBA (S-methylbenzylamine) salt useful as an intermediate in the manufacture of a glucokinase activator. As an overview of this scheme, a monohalogenated, cyclic, ketalized ketone is prepared using monohalogenation methodologies of the present invention. The halogenated compound is then subjected to a Favorskii rearrangement under conditions to provide the racemic acid counterpart of the desired chiral salt. The desired chiral salt is readily recovered in enantiomerically pure form from the racemic mixture.