📜Propargyl Monobromoacetate置于2,4,6-三甲基吡啶,二苯甲酮体系中,用 甲醇,异丙醇 作为反应溶剂,以40%的收率获得产物乙酸炔丙酯 参考文献:Unsaturated Spiro-γ-Lactone Formation By The Dissociative Reduction Of Bromoacetates 标题:Unsaturated Spiro-γ-Lactone Formation By The Dissociative Reduction Of Bromoacetates 摘要:Unsaturated Spiro-Gamma-Butyrolactones Can Be Prepared In Good Yields From Bromoacetate Precursors By A Simple Route That Requires Only 2-Propanol As Solvent And Free Radical Initiation. DOI:10.1016/s0040-4039(00)97292-7
专利号:US-2003180804-A1 优先权日:2001-10-29 标题:Solid phase synthesis of chemical libraries 发明人:PRYOR KENT E; LEWIS RONALD D; BROWN JASON W 权利人:CORVAS INT INC 摘要:The present invention provides compounds and compound libraries that are useful as protease modulators. The compounds and compound libraries are preferably made using the methods of the present invention which utilize peptide synthesis and combinatorial chemistry methods on a solid phase.
专利号:US-2005119332-A1 优先权日:1998-03-12 标 题 :Substituted thiophene compounds as modulators of protein tyrosine phosphatases (PTPases) 发明人:JEPPESEN LONE; ANDERSEN HENRIK S; OLSEN OLE H; JUDGE LUKE M; HOLSWORTH DANIEL D; BAKIR FARID; AXE FRANK U; GE YU 摘要:The present invention provides novel compounds of formula 1a, n nnovel 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. 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-2002165398-A1 优先权日:1998-03-12 标题:Modulators of protein tyrosine phosphatases (PTPases) 发明人:JEPPESEN LONE; ANDERSEN HENRIK SUNE; OLSEN OLE HVILSTED; JUDGE LUKE MILBURN; HOLSWORTH DANIEL DALE; BAKIR FARID; AXE FRANK URBAN; GE YU 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 Alzheimers disease and schizophrenia, and infectious diseases.
专利号:US-8829184-B2 优先权日:2010-04-15 标题:Intermediates useful for the synthesis of pyrrolobenzodiazepines 发明人:HOWARD PHILIP WILSON; MASTERSON LUKE; TIBERGHIEN ARNAUD 权利人:HOWARD PHILIP WILSON; MASTERSON LUKE; TIBERGHIEN ARNAUD; SPIROGEN SARL 摘要:A compound of formula (I): which is substantially free of any of the corresponding compound of formula (IB): methods of making such compounds, and the further transformation of such compounds.
专利号:US-3635999-A 优先权日:1969-03-25 标 题 :Synthesis of oxazoles 发明人:TRAMIER BERNARD; BONZOM ALBERT 权利人:AQUITAINE PETROLE 摘要:WHERE R2 IS ALKYL OF 1 TO 6 CARBON ATOMS, PHENYL OR HYDROXYPHENYL, R4 IS METHYL AND R5 IS HYDROGEN. A PROCESS OF PREPARING OXAZOLES IS DISCLOSED COMPRISING CONDENSING AN ACETYLENIC COMPOUND HAVING AN ELECTRONEGATIVE GROUP ON THE CARBON ATOM IN THE X-POSITION RELATIVE TO THE TRIPLE BOND WITH AN AMMONIUM SALT OF AN ORGANIC ACID OR AN AMIDE. 2-R2,4-R4,5-R5-OXAZOLE NEW OXAZOLES ARE PREPARED HAVING THE FORMULA
专利号:US-8269047-B2 优先权日:2009-07-23 标题 :Synthesis of alpha-halo enones and enals 发明人:ZHANG LIMING; YE LONGWU 权利人:ZHANG LIMING; YE LONGWU; UNIV NEVADA 摘要:A method for preparing an α-halo enal or enone from an unprotected propargyl alcohol and an electrophilic halogen source catalyzed by the combination of a gold catalyst complex and a metal co-catalyst complex is disclosed. The method can be further enhanced by addition of an additive that facilitates suppression of a des-halo derivative.
参考标题:Synthesis Of Piperidine Derivatives By Rhodium- Catalyzed Tandem Reaction OfN-Sulfonyl-1,2,3-Triazole And Vinyl Ether 作者:Sisi Yu,Yuehui An,Wenlin Wang,Ze-Feng Xu,Chuan-Ying Li |发布日期:2018.6.5 摘要:A Chemoselective Tandem Reaction Of 4‐acyloxymethylene‐1‐sulfonyl‐1,2,3‐triazole And Vinyl Ether Was Reported, Producing Polysubstituted Piperidine Derivatives In Up To 96% Yield. The Key Intermediate N‐sulfonyl 1‐azadiene Generated By Migration Of The Oac Group To The α‐imino Rhodium Carbene Was Isolated And A Plausible Mechanism Was Proposed. Several Related Ring Systems Were Constructed From The
合成参考文献
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