氰乙酸甲酯置于氨,甲烷体系中,用 甲醇 用作溶剂,化学反应 2.0H,反应生成氰乙酰胺 参考文献: Boron Containing Polybasic Bacterial Efflux Pump Inhibitors And Therapeutics Uses Thereof[fr] Inhibiteurs Des Pompes à Efflux Bactériennes Polybasiques Contenant Du Bore Et Utilisations Thérapeutiques De Ces Derniers 标题: Boron Containing Polybasic Bacterial Efflux Pump Inhibitors And Therapeutics Uses Thereof[fr] Inhibiteurs Des Pompes à Efflux Bactériennes Polybasiques Contenant Du Bore Et Utilisations Thérapeutiques De Ces Derniers 摘要:本文披露了含硼酸功能的多碱性细菌外流泵抑制剂及其合成方法,使用方法和药物组合物.一些实施例包括通过向感染细菌或有细菌感染风险的受试者共同给予外流泵抑制剂和另一种抗菌剂的方法来治疗或预防细菌感染.
专利信息
专利号:US-6136984-A 优先权日:1996-04-22 标 题 :Solid phase and combinatorial synthesis of substituted thiophenes and of arrays of substituted thiophenes 发明人:DOERWALD FLORENCIO ZARAGOZA 权利人:NOVO NORDISK AS 摘要:A solid phase method for the synthesis of a plurality of differently substituted thiophenes with a wide variety of side-chain substituents as compounds of potential therapeutic interest is disclosed. The thiophenes 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, followed by Thorpe-Ziegier-cyclization yields differently substituted, support-bound 3-aminothiophenes. These may be screened on the substrate or cleaved from the substrate and then screened in solution. Alternatively, the resin-bound 3-amino thiophenes or the synthetic intermediates can be subjected to further synthetic transformations (N-acylation, reduction) on the support, which permits the preparation of further therapeutically interesting compounds. The efficient synthesis of a wide variety of thiophenes using automated synthesis technology of the present method makes these compounds attractive candidates for the generation and rapid screening of diverse thiophene-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-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-7872143-B2 优先权日:2007-06-11 标题 :Facile synthesis of a series of liquid crystalline 2-(4′-alkoxyphenyl)-5-cyanopyridines 发明人:CHIA WIN-LONG; CHENG YU-WEI 权利人:UNIV FU JEN CATHOLIC 摘要:The invention relates to a facile synthesis of a series of 2-(4′-alkoxyphenyl)-5-cyanopyridine liquid crystal compounds which are represented by the following formula (I): n n n n n n n n n n wherein C n H 2n+1 is a linear alkyl group having 2-12 carbon atoms. The synthesis of the liquid crystalline 2-(4′-alkoxyphenyl)-5-cyanopyridine is completed in a two-step reaction. First, a Grignard reagent (such as 4-alkoxyphenylmagnesium bromide) is added to a 3-cyanopyridinium salt (such as N-phenyloxycarbonyl-3-cyanopyridinium chloride) to get a 1,2-dihydropyridine. Then, the 1,2-dihydropyridine is oxidized with o-chloronil to obtain the 2-(4′-alkoxyphenyl)-5-cyanopyridine.
专利号:US-7465802-B2 优先权日:2006-12-13 标 题:Facile synthesis of a series of liquid crystalline 2-(4′-alkylphenyl)-5-cyanopyridines 发明人:CHIA WIN-LONG; LU RU-SUNG 权利人:UNIV FU JEN CATHOLIC 摘要:The invention relates to a facile synthesis of a series of 2-(4′-alkylphenyl)-5-cyanopyridine liquid crystal compounds which are represented by the following formula (I): n nwherein C n is a linear alkyl having 1-12 carbon atoms. The synthesis of the liquid crystalline 2-(4′-alkylphenyl)-5-cyanopyridine is completed in a two-step reaction. First, a Grignard reagent (such as 4-alkylphenylmagnesium bromide) is added to a 3-cyanopyridinium salt (such as N-phenyloxycarbonyl-3-cyanopyridinium chloride) to get a 1,2-dihydropyridine. Then the 1,2-dihydropyridine is oxidized with o-chloronil to obtain the 2-(4′-alkylphenyl)-5-cyanopyridine.
专利号:US-4866175-A 优先权日:1966-11-08 标 题 :Novel process for the synthesis of quinoxaline and benzimidazole-N-oxides 发明人:ISSIDORIDES COSTAS H; HADDADIN MAKHLUF J 权利人:RESEARCH CORP 摘要:The synthesis of quinoxaline and benzimidazole-N-oxides and of ester amd amide derivatives of 3-hydroxy-2-quinoxalinecarboxylic acid by a movel process consisting of the reaction between a benzofuroxan and an activated methylene-containing compound under basic conditions.
专利号:US-2012149895-A1 优先权日:2009-04-01 标题 :Process for dimethylation of active methylene groups 发明人:JENKO BRANKO; COPAR ANTON 权利人:JENKO BRANKO; COPAR ANTON; LEK PHARMACEUTICALS 摘要:The present invention discloses a process for dimethylation of active methylene groups. Specifically, the invention discloses a process for preparing 3-amino-2,2-dimethylpropanamide. Compounds produced by the present dimethylation process such as 3-amino-2,2-dimethylpropanamide can be used as intermediates in the route of synthesis of therapeutic, prophylactic or diagnostic agent, for example aliskiren or cryptophycin. Particularly, the invention relates to embodiments further extending to processes for preparing pharmaceutical dosage form comprising said therapeutic, prophylactic or diagnostic agents. More specifically, the invention relates to the use of compounds produced by the present dimethylation process for the manufacture of therapeutic, prophylactic or diagnostic agents or for the manufacture of pharmaceutical dosage forms comprising said therapeutic, prophylactic or diagnostic agents. The processes according to the present invention can be beneficially applied for the synthesis of various active pharmaceutical ingredients, such as aliskiren or crypthophycin.
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合成参考文献
参考文献:10.4103/0971-4065.82131 摘要:Boutabet K, Kebsa W, Alyane M, Lahouel M. Polyphenolic fraction of Algerian propolis protects rat kidney against acute oxidative stress induced by doxorubicin. Indian J Nephrol. 2011 Apr;21(2):101–6.