专利号:US-6376676-B1 优先权日:1993-06-30 标题 :Intermediates in the synthesis of (±)-camptothecin and related compounds and synthesis thereof 发明人:CURRAN DENNIS P; LIU HUI 权利人:UNIV PITTSBURGH 摘要:The present invention provides a short, convergent total synthesis of novel intermediates in the synthesis of (±)-camptothecin and related compounds. The present synthesis scheme includes a novel 4+1 radical annulation followed by another cyclization to simultaneously assemble rings B and C of the camptothecin compound. The present invention also provides novel chemical intermediates for such 4+1 radical annulations.
专利号:US-6252079-B1 优先权日:1993-06-30 标 题 :Intermediates in the synthesis of camptothecin and related compounds and synthesis thereof 发明人:CURRAN DENNIS P; BOM DAVID 权利人:UNIV PITTSBURGH 摘要:The present invention provides a short, convergent total synthesis of irinotecan and derivative compounds which comprises of a novel 4+1 radical annulation wherein the precursoris reacted with an aryl isonitrile having the formulawherein X is Br or I, and R4 is an alkyl group, an allyl group, a propargyl group or a benzyl group, and R16 is H, a C1-C6 alkoxy group, agroup wherein p is an integer between 4 and 12, or a C1-C12 acyclic dialkylamino group. The present invention also provides novel chemical intermediates for such 4+1 radical annulations.
专利号:US-6982333-B2 优先权日:1993-06-30 标 题:Intermediates in the synthesis of camptothecin and related compounds and synthesis thereof 发明人:CURRAN DENNIS P; JOSIEN HUBERT; KO SUNG BO 权利人:UNIV PITTSBURGH 摘要:The present invention provides a short, convergent total synthesis of camptothecin and related compounds which consists of a novel 4+1 radical annulation. The present invention also provides novel chemical intermediates for such 4+1 radical annulations.
专利号:US-3886180-A 优先权日:1973-03-15 标 题:Process for the synthesis of N-hydroxypyrroles 发明人:ABRAMOVITCH RUDOLPH ABRAHAM; CUE JR BERKELEY WENDELL 权利人:ABRAMOVITCH RUDOLPH ABRAHAM; CUE JR BERKELEY WENDELL 摘要:A process is described for the preparation of N-hydroxypyrrole2-carbonitriles, N-hydroxyimidazole-2-carbonitriles, pyrrole-2carbonitriles, and 3-substituted-2, 3-dihydro-2-pyrrolones by thermally decomposing 2-azidoheteroaromatic N-oxides. In the process a 2-azidoheteroaromatic N-oxide is heated in a suitable solvent for a period of time sufficient to bring the reaction to completion. Removal of the solvent by conventional methods gives the desired product. Which product is obtained is determined by the choice of solvents. In non-polar aprotic solvents, Nhydroxypyrrole-2-carbonitriles or N-hydroxyimidazole-2carbonitriles are obtained. In nucleophilic solvents capable of undergoing Michael-type additions pyrrole-2-carbonitriles, imidazole-2-carbonitriles, and 3-substituted-2,3-dihydro-2pyrrolone derivatives are obtained where a solvent molecule comprises the 3-substituent. These compounds are useful as antibaterials, e.g., against E. Coli.
专利号:US-4006160-A 优先权日:1973-03-15 标题:Process for the synthesis of N-hydroxypyrroles, N-hydroxyimidazoles, and derivatives thereof 发明人:ABRAMOVITCH RUDOLPH ABRAHAM; CUE JR BERKELEY WENDELL 权利人:UNIV ALABAMA 摘要:A process is described for the preparation of N-hydroxypyrrole-2-carbonitriles, N-hydroxyimidazole-2-carbonitriles, pyrrole-2-carbonitriles, and 3-substituted-2, 3-dihydro-2-pyrrolones by thermally decomposing 2-azidoheteroaromatic N-oxides. In the process a 2-azidoheteroaromatic N-oxide is heated in a suitable solvent for a period of time sufficient to bring the reaction to completion. Removal of the solvent by conventional methods gives the desired product. Which product is obtained is determined by the choice of solvents. In non-polar aprotic solvents, N-hydroxypyrrole-2-carbonitriles or N-hydroxyimidazole-2-carbonitriles are obtained. In nucleophilic solvents capable of undergoing Michael-type additions pyrrole-2-carbonitriles, imidazole-2-carbonitriles, and 3-substituted-2,3-dihydro-2-pyrrolone derivatives are obtained where a solvent molecule comprises the 3-substituent. These compounds are useful as anti-bacterials, e.g., against E. Coli.
专利号:US-2004063947-A1 优先权日:1993-06-30 标 题:Novel intermediates in the synthesis of camptothecin and related compounds and synthesis thereof
摘要:Calleja, P.; Dorel, R.; Echavarren, A. M., Science of Synthesis: Catalytic Oxidation in Organic Synthesis, (2017) 1, 497. 摘要:Calleja, P.; Dorel, R.; Echavarren, A. M., Science of Synthesis: Catalytic Oxidation in Organic Synthesis, (2017) 1, 520. 摘要:Calleja, P.; Dorel, R.; Echavarren, A. M., Science of Synthesis: Catalytic Oxidation in Organic Synthesis, (2017) 1, 490.