专利号:US-8822702-B2 优先权日:2002-12-20 标 题 :Synthesis of amines and intermediates for the synthesis thereof 发明人:BERENS ULRICH; DOSENBACH OLIVER; SPRENGER DANIEL 权利人:BERENS ULRICH; DOSENBACH OLIVER; SPRENGER DANIEL; BASF SE 摘要:The invention relates in a first embodiment to a method for the manufacture of esters of the formula I, n nor especially of amides of the formula II,n n nwherein the symbols have the meanings given in the specification, as well as other intermediates and compounds useful in the synthesis of tryptamines and other substances mentioned in the title. The synthesis methods and intermediates are useful in the synthesis of pharmaceuticals.
专利号:EP-0791575-A1 优先权日:1996-02-16 标题 :Method of synthesis of a quaternary ammonium salt 发明人:NAKANO SHINJI 权利人:NIPPON PAINT CO LTD 摘要:The present invention provides an improved method of synthesis of a quaternary ammonium salt in which a tertiary amine is reacted with a benzyl halide optionally having on the benzene ring and/or at the α-site one ore more substituent groups inert to the reaction, which method is characterized in that the reaction is carried out in water or in a water-containing organic solvent.
专利号:US-7786156-B2 优先权日:2004-01-28 标 题 :Synthesis methods and intermediates for the manufacture of Rizatriptan 发明人:MARTIN PIERRE; BERENS ULRICH; BOUDIER ANDREAS; DOSENBACH OLIVER 权利人:RATIOPHARM GMBH 摘要:The invention relates to a process for the manufacture of an 1,2,4-triazol-1-yl compound of the formula [A], n nor a salt thereof, wherein each of R3 and R4 is hydrogen or lower alkyl, said process comprising reacting a hydrazine compound of the formula [B]n n nwherein R is hydrogen or acyl, R2 is hydrogen or a protecting group, are hydrogen or lower alkyl, and R6 is hydrogen or COOR7, or a salt thereof, with a 1,2,4-triazolyl forming reagent.n n In addition, novel intermediates for the synthesis of the anti-migraine agent Rizatriptan and methods for their synthesis are presented.
专利号:US-8309695-B2 优先权日:2007-06-11 标题 :Marking reagents bearing diazo and nitro functions, methods for the synthesis of such reagents and methods for detecting biological molecules 发明人:LAURENT ALAIN; LAAYOUN ALI; KOTERA MITSUHARU 权利人:LAURENT ALAIN; LAAYOUN ALI; KOTERA MITSUHARU; BIOMERIEUX SA; CENTRE NAT RECH SCIENT; UNIV STRASBOURG 摘要:The present invention relates to a labeling reagent of formula: n nin which:n R 1 represents at least one detectable label, L and A are each a linker arm, n is an integer equal to 1, and u is an integer between 0 and 2.n nThe present invention also describes a method of synthesizing said markers and also applications for the labeling of biological molecules, more particularly nucleic acids, with a labeling reagent bearing diazo and nitro functions. The invention is particularly suitable for use in the diagnostics field.
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.