专利号:US-6251689-B1 优先权日:1998-05-14 标 题:Methods for the solid phase synthesis of combinatorial libraries of benzimidazoles benzoxazoles benzothiazoles and derivatives thereof 发明人:LABORDE EDGARDO; MATSUMOTO YUKIHARU 权利人:TELIK INC 摘要:The present invention provides an efficient and versatile method for the synthesis and screening of combinatorial libraries of benzimidazoles, benzoxazoles, benzothiazoles, and derivatives thereof. In order to expedite the synthesis of large arrays of compounds possessing these core structures, a general methodology for solid phase synthesis of these derivatives is provided. Arrays of benzimidazoles, benzoxazoles, benzothiazoles, and derivatives thereof useful as peptidomimetics and for the identification of agents having antifungal, antiviral, antimicrobial, anticoagulant, and antiulcer activity, or use in the treatment of inflammation, hypertension, cancer, and other conditions can be prepared by this method.
专利号:US-5861532-A 优先权日:1997-03-04 标 题:Solid-phase synthesis of N-alkyl amides 发明人:BROWN EDWARD G; NUSS JOHN M 权利人:CHIRON CORP 摘要:Methods for solid phase synthesis of N-alkyl amides comprise reductive amination of carbonyl compounds using a reducing agent and an amine-containing linker bound to a solid support. The methods afford high yields of linker-bound, monoalkylated amines, and subsequent coupling with acid derivatives provide derivatized N-substituted amides in excellent yields after cleavage from the solid-phase. Compositions useful in solid phase synthesis are also described.
专利号:US-4582903-A 优先权日:1984-08-17 标 题 :Synthesis of unsaturated hydantoins with an inexpensive catalyst 发明人:MIRVISS STANLEY B 权利人:STAUFFER CHEMICAL CO 摘要:Alkylidene or arylidene substituted hydantoins are produced by condensation of an aromatic or aliphatic aldehyde with hydantoin in the presence of at least one basic salt of an inorganic acid. The desired products are obtained in high yields.
专利号:CN-104804003-A 优先权日:2015-04-27 标题 :Synthesis of 5-aryl-1H-pyrazolo[4,3-d]pyrimidin-7(6H)-one
专利号:US-8558012-B2 优先权日:2009-03-02 标 题:2-fluoro-1,3-benzodithiol 1,1,3,3-tetraoxide derivative, production method thereof, and production method of monofluoromethyl group-containing compound using the same 发明人:SHIBATA NORIO 权利人:SHIBATA NORIO; NAGOYA INST TECHNOLOGY; TOSOH P TECH INC 摘要:A 2-fluoro-1,3-benzodithiol 1,1,3,3-tetraoxide derivative as a monofluoromethyl group introduction agent that is effective as an intermediate in pharmaceutical and agrochemical synthesis, a production method thereof, and a production method of a monofluoromethyl group-containing compound using this 2-fluoro-1,3-benzodithiol 1,1,3,3-tetraoxide derivative are provided. The 2-fluoro-1,3-benzodithiol 1,1,3,3-tetraoxide derivative represented by the following general formula (1) (wherein R 1 , R 2 , R 3 , and R 4 each independently represent a hydrogen atom, a straight-chain or branched alkyl group having 1 to 4 carbon atoms, a straight-chain or branched alkyloxy group having 1 to 4 carbon atoms, a halogen atom, a nitro group, or a cyano group), the production method thereof, and various monofluoromethyl group-containing compounds are manufactured using this 2-fluoro-1,3-benzodithiol 1,1,3,3-tetraoxide derivative as a monofluoromethylating agent.
专利号:US-2001024833-A1 优先权日:1998-05-14 标 题 :Methods for the solid phase synthesis of combinatorial libraries of benzimidazol, benzoxazoles, benzothiazoles, and derivatives thereof
参考标题:Design And Synthesis Of Low Molecular Weight Compounds With Complement Inhibition Activity 作者:Hoshang E. Master,Shabana I. Khan,Krishna A. Poojari |发布日期:2005.8 摘要:An Attempt Was Made To Synthesize A Series Of Non-Cytotoxic Low Molecular Weight Compounds Of Varying Substitutions And Functionalities Having Pharmacophore Activity Like Carbonyl Compounds, Carboxylic Acid And Bioisosteres Like Tetrazole And Phenyl Acrylic Acid. The In Vitro Assay Of These Analogues For The Inhibition Of Complement Activity Revealed Significant Inhibitory Activity For Varying Substituents
合成参考文献
参考文献:10.1107/s1600536810019951 摘要:Ge CM, Zhang SH, Chao F, Wang YG, Li W. 2-Eth-oxy-6-[(methyl-imino)-meth-yl]phenol. Acta Crystallogr Sect E Struct Rep Online. 2010 Jun 05;66(Pt 7):o1526. 参考文献:10.1107/s1600536810040043 摘要:Huang YD, Zhang S, Qin JK, Chen FL. Tris[2-ethoxy-6-(methyliminomethyl)phenolato-κ2N,O1]cobalt(III) monohydrate. Acta Crystallogr E Struct Rep Online. 2010 Oct 13;66(11):m1399. doi: 10.1107/s1600536810040043.