苄氧羰基-L-丙氨酰-L-脯氨酸置于10% Palladium On Active Carbon 溶剂黄146体系中,用 甲醇 用作溶剂,化学反应 2.0H,以98%的收率获得l-丙氨酰基-L-脯氨酸 参考文献:Synthesis And Nootropic Activity Of Pyrrolidino[1,2-A]Diazacycloalkanes 标题:Synthesis And Nootropic Activity Of Pyrrolidino[1,2-A]Diazacycloalkanes 摘要: Doi:10.1007/bf02219346
专利号:WO-2004046173-A1 优先权日:2002-11-19 标题:Scaffolds useful to the synthesis of compounds with biological activity 发明人:GIANNINI GIUSEPPE; SCOLASTICO CARLO; MANZONI LEONARDO 权利人:SIGMA TAU IND FARMACEUTI; GIANNINI GIUSEPPE; SCOLASTICO CARLO; MANZONI LEONARDO 摘要:The present invention relates to cyclic compounds having the azabicycloalkane structure. Said compounds are useful as intermediates for the synthesis of compounds with biological activity.
专利号:US-5714127-A 优先权日:1992-10-08 标题 :System for multiple simultaneous synthesis 发明人:DEWITT SHEILA H H; KIELY JOHN S; PAVIA MICHAEL R; SCHROEDER MEL C; STANKOVIC CHARLES J 权利人:WARNER LAMBERT CO 摘要:A system for the multiple, simultaneous synthesis of compounds preferably uses a reaction apparatus comprising a reservoir rack having a plurality of reaction wells, a plurality of reaction tubes, usually gas dispersion tubes, having filters on their lower ends, a holder block, having a plurality of apertures, and a manifold, which has ports to allow introduction/maintenance of a controlled environment. The manifold top wall has a plurality of apertures in axial alignment with the reaction tubes and a gasket which allows penetration by a needle in order to dispense and aspirate materials from the reaction tubes. Sealing members, such as gaskets, are placed between the holder block, manifold and reservoir rack and the components are releasably fastened together. A robotic sample processor is used to automate the synthesis process using the reaction apparatus.
专利号:US-5702672-A 优先权日:1992-10-08 标 题 :Apparatus and method for multiple simultaneous synthesis 发明人:DEWITT SHEILA H H; KELL MICHAEL; PAVIA MICHAEL R; KIELY JOHN S; SCHROEDER MEL C; STANKOVIC CHARLES J; WARE STEVEN 权利人:WARNER LAMBERT CO 摘要:An apparatus for multiple, simultaneous synthesis of compounds which consists of: a reservoir block having a plurality of wells; a plurality of reaction tubes, usually gas dispersion tubes, having filters on their lower ends; a holder block, having a plurality of apertures; and a manifold, which may have ports to allow introduction/maintenance of a controlled environment. The manifold top wall has apertures and a detachable plate with identical apertures. The apparatus is constructed from materials which will accommodate heating, cooling, agitation, or corrosive reagents. Gaskets are placed between the components. Rods or clamps are provided for fastening the components together. Apparatus operation involves placing the filters on the lower ends of the reaction tubes in the reservoir block wells, and the upper ends passing through the holder block apertures and into the manifold.
专利号:US-5766556-A 优先权日:1992-10-08 标题:Apparatus and method for multiple simultaneous synthesis 发明人:DEWITT SHEILA HELEN HOBBS; KIELY JOHN STEVEN; PAVIA MICHAEL RAYMOND; SCHROEDER MEL CONRAD; STANKOVIC CHARLES JOHN 权利人:WARNER LAMBERT CO 摘要:An apparatus and method which provides a suitable location for multiple, simultaneous synthesis of compounds. The apparatus consists of: a reservoir block having a plurality of wells; a plurality of reaction tubes, usually gas dispersion tubes, having filters on their lower ends; a holder block, having a plurality of apertures; and a manifold, which may have ports to allow introduction/maintenance of a controlled environment. The manifold top wall has apertures and a detachable plate with identical apertures. The apparatus is constructed from materials which will accommodate heating, cooling, agitation, or corrosive reagents. Gaskets are placed between the components. Rods or clamps are provided for fastening the components together. Apparatus operation involves placing the filters on the lower ends of the reaction tubes in the reservoir block wells, and the upper ends passing through the holder block apertures and into the manifold. The apparatus provides in excess of 1 mg of each product with structural knowledge and control over each compound. The apparatus can be adapted to manual, semiautomatic or fully automatic performance. Using the apparatus a series of building blocks are covalently attached to a solid support. These building blocks are then modified by covalently adding additional different building blocks or chemically modifying some existing functionality until the penultimate structure is achieved. This is then cleaved from the solid support by another chemical reaction into the solution within the well yielding an array of newly synthesized individual compounds, which after postreaction modification, if necessary, are suitable for testing for activity.
专利号:US-5567391-A 优先权日:1992-10-08 标题 :Apparatus for multiple simultaneous synthesis 发明人:DEWITT SHEILA H H; KIELY JOHN S; PAVIA MICHAEL R; SCHROEDER MEL C; STANKOVIC CHARLES J 权利人:WARNER LAMBERT CO 摘要:An apparatus and method which provides a suitable location for multiple, simultaneous synthesis of compounds. The apparatus consists of: a reservoir block having a plurality of wells; a plurality of reaction tubes, usually gas dispersion tubes, having filters on their lower ends; a holder block, having a plurality of apertures; and a manifold, which may have ports to allow introduction/maintenance of a controlled environment. The manifold top wall has apertures and a detachable plate with identical apertures. The apparatus is constructed from materials which will accommodate heating, cooling, agitation, or corrosive reagents. Gaskets are placed between the components. Rods or clamps are provided for fastening the components together. Apparatus operation involves placing the filters on the lower ends of the reaction tubes in the reservoir block wells, and the upper ends passing through the holder block apertures and into the manifold. The apparatus provides in excess of 1 mg of each product with structural knowledge and control over each compound. The apparatus can be adapted to manual, semiautomatic or fully automatic performance. Using the apparatus a series of building blocks are covalently attached to a solid support. These building blocks are then modified by covalently adding additional different building blocks or chemically modifying some existing functionality until the penultimate structure is achieved. This is then cleaved from the solid support by another chemical reaction into the solution within the well yielding an array of newly synthesized individual compounds, which after postreaction modification, if necessary, are suitable for testing for activity.
专利号:US-7183396-B2 优先权日:1999-06-15 标题:Linvin, a novel inhibitor of apoptosis protein 发明人:GOMES BRUCE C; KASOF GARRETT M; PROSSER JUDITH C 权利人:GOMES BRUCE C; KASOF GARRETT M; PROSSER JUDITH C 摘要:A novel isolated and purified human protein inhibitor of apoptosis, termed livin, is described. A cDNA sequence which encodes the native inhibitor of apoptosis (livin) is disclosed as well as the structural coding region and the amino acid residue sequence. Molecular sequences are provided for the design and synthesis of entities that modulate biological and/or pharmacological activity of the native biomolecule. Methods are provided which employ the sequences to identify compounds that modulate biological and/or pharmacological activity of the native biomolecule. Biologically-effective antisense molecules as well as dominant negative mutant versions of the livin protein which are suitable for therapeutic are also provided. The invention is also drawn toward the study, prevention, diagnosis, and treatment of pathophysiological disorders related to apoptosis.
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合成参考文献
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