专利号:WO-2009152051-A1 优先权日:2008-06-12 标题:Synthesis of a macrocyclic hcv protease inhibitor 发明人:WANG PENG 权利人:PHENOMIX CORP; WANG PENG 摘要:The present invention provides a method of synthesis of a macrocyclic compound known as a potent inhibitor of a protease produced by the hepatitis C virus (HCV). Inhibition of the viral protease blocks assembly of mature viral particles in an infected mammalian host. The method of synthesis involves a ring-closing metathesis step using a ruthenium catalyst. Hydrogenation and boronate deprotection provide the HCV protease-inhibitory product.
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:WO-9630393-A1 优先权日:1995-03-27 标 题:A method for the synthesis of mixtures of compounds 发明人:BECKER KATHERINE; DEWITT SHEILA HOBBS 权利人:WARNER LAMBERT CO 摘要:Described is a method of synthesizing a plurality of compounds in a plurality of wells comprising the steps of: (a) providing a plurality of test wells in a plurality of arrays of the wells; (b) reacting in at least a one step reaction a first reagent with a plurality of reagents called building blocks in the test well to obtain a unique product designed to be the same in each array; and (c) continuing to react reagents such that there are multiple reagents resulting in mixtures of multiple different products in each well.
摘要:Spitzner, D., Science of Synthesis Knowledge Updates, (2016) 1, 248. 摘要:Kleoff, M.; Omoregbee, K.; Zimmer, R., Science of Synthesis Knowledge Updates, (2018) 4, 218. 参考文献:10.1155/s1565363303000189 摘要:Xanthopoulou MN, Hadjikakou SK, Hadjiliadis N, Schürmann M, Jurkschat K, Binolis J, Karkabounas S, Charalabopoulos K. Communication: Synthesis of a Novel Triphenyltin(IV) Derivative of 2‐Mercaptonicotinic Acid with Potent Cytotoxicity in vitro. Bioinorganic Chemistry and Applications. 2003 Jan;1(3-4):227–31. doi: 10.1155/s1565363303000189. 参考文献:10.1107/s1600536810048385 摘要:Jiang XR, Wang XJ, Feng YL. 4,4'-Bipyridine-2-(carb-oxy-methyl-sulfan-yl)pyridine-3-carb-oxy-lic acid (1/1). Acta Crystallogr Sect E Struct Rep Online. 2010 Nov 27;66(Pt 12):o3308.