📜溴苯乙腈,硫脲 反应生成 阿米苯唑 参考文献:Davies Et Al.,Journal Of The Chemical Society,1950,P. 3491,3494 标题:Davies Et Al.,Journal Of The Chemical Society,1950,P. 3491,3494
专利号:US-5847150-A 优先权日:1996-04-24 标题 :Solid phase and combinatorial synthesis of substituted 2-methylene-2, 3-dihydrothiazoles and of arrays of substituted 2-methylene-2, 3-dihydrothiazoles 发明人:DORWALD FLORENCIO ZARAGOZA 权利人:NOVO NORDISK AS 摘要:A solid phase method for the synthesis of a plurality of differently substituted 2-methylenethiazoles with a wide variety of side-chain substituents as compounds of potential therapeutic interest. The 2-methylenethiazoles are prepared by acylation of a substrate-bound primary or secondary amine with cyanoacetic acid and reaction of the resulting cyanoacetamide with an isothiocyanate in the presence of a base. Alkylation with an appropriate alkyl halide under acidic conditions yields differently substituted, support-bound 2-methylene-2,3-dihydrothiazoles. These may be screened on the substrate or cleaved from the substrate and then screened in solution. The efficient synthesis of a wide variety of 2-methylenethiazoles using automated synthesis technology of the present method makes these compounds attractive candidates for the generation and rapid screening of diverse thiazole-based libraries. The method disclosed here provides an easy and fast access to highly diverse heterocyclic compounds of therapeutic interest, amenable to automatization.
专利号:US-6531470-B1 优先权日:1998-01-23 标题:Oxazolidinone combinatorial libraries, compositions and methods of preparation 发明人:GORDEEV MIKHAIL F; LUEHR GARY W; PATEL DINESH V; NI ZHI-JIE; GORDON ERIC 权利人:UPJOHN CO 摘要:Oxazolidinones and methods for their synthesis are provided. Also provided are combinatorial libraries comprising oxazolidinones, and methods to prepare the libraries. Further provided are methods of making biologically active oxazolidinones as well as pharmaceutically acceptable compositions comprising the oxazolidinones. The methods of library preparation include the attachment of oxazolidinones to a solid support. The methods of compound preparation in one embodiment involve the reaction of an iminophosphorane with a carbonyl containing polymeric support.
专利号:US-6562844-B2 优先权日:1998-01-23 标 题:Oxazolidinone combinatorial libraries, compositions and methods of preparation 发明人:GORDEEV MIKHAIL F; LUEHR GARY W; PATEL DINESH V; NI ZHI-JIE; GORDON ERIC 权利人:UPJOHN CO 摘要:Oxazolidinones and methods for their synthesis are provided. Also provided are combinatorial libraries comprising oxazolidinones, and methods to prepare the libraries. Further provided are methods of making biologically active oxazolidinones as well as pharmaceutically acceptable compositions comprising the oxazolidinones. The methods of library preparation include the attachment of oxazolidinones to a solid support. The methods of compound preparation in one embodiment involve the reaction of an iminophosphorane with a carbonyl containing polymeric support.
专利号:WO-9740030-A1 优先权日:1996-04-24 标 题:Solid phase and combinatorial synthesis of substituted 2-methylene-2,3-dihydrothiazoles and of arrays of substituted 2-methylene-2,3-dihydrothiazoles
专利号:US-7002020-B1 优先权日:1998-01-23 标题:Oxazolidinone combinatorial libraries, compositions and methods of preparation 发明人:GORDEEV MIKHAIL F; LUEHR GARY W; PATEL DINESH V 权利人:UPJOHN CO 摘要:Oxazolidinones and methods for their synthesis are provided. Also provided are combinatorial libraries comprising oxazolidinones, and methods to prepare the libraries. Further provided are methods of making biologically active oxazolidinones as well as pharmaceutically acceptable compositions comprising the oxazolidinones. The methods of library preparation include the attachment of oxazolidinones to a solid support. The methods of compound preparation in one embodiment involve the reaction of an iminophosphorane with a carbonyl containing polymeric support.
专利号:CN-106458847-B 优先权日:2014-05-29 标 题:Synthesis of Novel Diamine and Liquid Crystal Aligning Agent Using It
1: Lehmann KA, Huttarsch H, Schroeder B, Zech D. [Development of continuous monitoring of spontaneous respiration in the postoperative phase. 2. Cutaneous oxygen and carbon dioxide partial pressures following i.v. bolus application of fentanyl, buprenorphine, naloxone and amiphenazole in healthy adult subjects]. Anaesthesist. 1992 Apr;41(4):192-8. German. 4: Lehmann KA, Asoklis S, Grond S, Schroeder B. [Continuous monitoring of spontaneous postoperative respiration. 3. The effect of amiphenazole on cutaneous oxygen and carbon dioxide partial pressure following gynecologic surgery under halothane anesthesia]. Anaesthesist. 1993 Apr;42(4):227-31. German. 7: AMIPHENAZOLE and morphine. Br Med J. 1956 Jan 21;1(4959):161-2.
合成参考文献
摘要:S72 | NTUPHTW | Pharmaceutically Active Substances from National Taiwan University | DOI:10.5281/zenodo.3955664 摘要:Sidorowicz K, Tkacz E, Poloński L. [Influence of therapy schedule on hospitalization frequency and prognosis in heart failure in 3 yrs. observations]. Pol Merkur Lekarski. 2002 Jan;12(67):30–5.