专利号:WO-2016173960-A1 优先权日:2015-04-29 标 题 :Optimized synthesis of pregabalin and 4-aminobutane acid using an improved method for producing conjugated nitroalkenes 发明人:STUMPF MARCUS 权利人:K H S PHARMA HOLDING GMBH 摘要:The invention relates to an optimized synthesis of pregabalin and additional 4-aminobutane acids using an improved method for producing conjugated nitroalkenes. This is achieved by a nitro-aldol reaction of an aliphatic aldehyde with a nitroalkane in the presence of a suitable diamine directly followed by an elimination of the conjugated nitroalkene by adding an acid, a subsequent catalyzed asymmetrical 1,4-Michael addition of a suitable nucleophile, and a subsequent retro-Claisen reaction or a hydrolosis and decarboxylation with a concluding reduction to 4-aminobutane acid.
专利号:US-6835841-B2 优先权日:2002-09-13 标 题:Asymmetric catalytic hydrogenation process for preparation of chiral cyclic β-aminoesters 发明人:DEERBERG JOERG; MCLEOD DOUGLAS D; YUE TAI-YUEN 权利人:BRISTOL MYERS SQUIBB CO 摘要:A novel process for the asymmetric synthesis of substituted cyclic beta-amino-carboxylates of the type shown in the specification from appropriate beta-enamino-ester starting materials is described. These compounds are useful as intermediates for MMP and TACE inhibitors.
专利号:US-5879690-A 优先权日:1995-09-07 标题:Topical administration of catecholamines and related compounds to subcutaneous muscle tissue using percutaneous penetration enhancers 发明人:PERRICONE NICHOLAS V 摘要:Compositions for the topical treatment of sagging subcutaneous muscle and overlying cutaneous tissue contain an active ingredient exhibiting or producing catecholamine activity such as catecholamines and/or related compounds in a dermatologically acceptable carrier that contains at least one percutaneous penetration enhancer. Examplary catecholamines include adrenaline, norepinepherine, dopamine and their precursors; catecholamine precursors such as tyrosine and phenylalanine are preferred. Many embodiments, particularly those employing tyrosine and/or phenylalanine as a catecholamine precursor, further contain a neurotransmitter synthesis enhancer such as dimethylaminoethanol, and other co-factors such as vitamin B 6 and pantothenic acid or calcium pantothenate are included in the composition to enhance the action of the active ingredients. Other compounds that scavenge free radicals and antioxidants may also be added.
专利号:EP-3002290-A2 优先权日:2007-06-19 标 题 :Synthesis of deoxycholic acid (dca)
专利号:CA-2439836-A1 优先权日:2001-03-01 标 题 :Method for the synthesis of 2',3'-dideoxy-2',3'-didehydronucleosides
专利号:US-4511741-A 优先权日:1983-12-02 标题 :Production of aldehydes from organic acid esters 发明人:WEGMAN RICHARD W; BUSBY DAVID C 权利人:UNION CARBIDE CORP 摘要:A process for the production of an aldehyde at high selectivity and rate by the reaction of an organic ester with carbon monoxide or synthesis gas in contact with a catalyst system containing rhodium atoms and cobalt atoms and lithium iodide or lithium bromide and, optionally, an organic ligand.