专利号:US-9085538-B2 优先权日:2010-07-26 标题:Process for the preparation of key intermediates for the synthesis of statins or pharmaceutically acceptable salts thereof 发明人:CASAR ZDENKO; STERK DAMJAN; JUKIC MARKO 权利人:CASAR ZDENKO; STERK DAMJAN; JUKIC MARKO; LEK PHARMACEUTICALS 摘要:The invention relates to commercially viable process for the synthesis of key intermediates for the preparation of statins, in particular Rosuvastatin and Pitavastatin or respective pharmaceutically acceptable salts thereof. A new simple and short synthetic route for key intermediates is presented which benefits from the use of cheap and readily available starting materials, by which the conventionally most frequently used DIBAL-H as reducing agent can be avoided.
专利号:US-5998633-A 优先权日:1996-07-29 标 题:Process for the synthesis of protected esters of (S)-3,4-dihydroxybutyric acid 发明人:JACKS THOMAS E; BUTLER DONALD E 权利人:WARNER LAMBERT CO 摘要:The invention is an improved process for the preparation of a compound of formula I wherein R and R 1 are each independently alkyl of from 1 to 3 carbon atoms; and R 2 is alkyl of from 1 to 8 carbon atoms. ##STR1##
专利号:US-7737287-B2 优先权日:2002-03-28 标 题 :Anomeric derivatives of monosaccharides 发明人:MEUTERMANS WIM; WEST MICHAEL LEO; GIANG THANH LE; ADAMSON GEORGE; SCHAFER KARL; ABBENANTE GIOVANNI 权利人:ALCHEMIA LTD 摘要:This invention relates to combinatorial libraries of potentially biologically active mainly monosaccharide compounds and to methods of preparing same. These compounds are variously functionalized, with a view to varying lipid solubility, size, function and other properties, with the particular aim of discovering a drug or drug-like compound, or compounds with useful properties. The invention provides intermediates, processes and synthetic strategies for the solution or solid phase synthesis of monosaccharides, variously functionalized about the sugar ring, including the addition of aromaticity and charge, and the placement of amino acid and peptide side chain units of isosteres thereof.
专利号:US-5194671-A 优先权日:1991-05-23 标题 :Process for the preparation of β-ketocarboxylic acid esters 发明人:MEIER JOSEF 权利人:WACKER CHEMIE GMBH 摘要:The invention relates to a process for the preparation of β-ketocarboxylic acid esters of the general formula ##STR1## in which R 1 is an alkyl radical having 1 to 4 C atoms, R 2 is an alkyl radical or alkenyl radical having 2 to 15 C atoms or a phenyl radical and R 3 is hydrogen or an alkyl or alkenyl radical having 1 to 6 C atoms, characterized in that acetocarboxylic acid esters of the general formula ##STR2## in which R 1 and R 3 are as defined, are reacted with calcium hydroxide or calcium oxide in the presence of an organic solvent and in the absence of water, the calcium chelate complexes formed are acylated with carboxylic acid chloride and the products are then cleaved with aqueous ammonium salt solution to form the β-ketocarboxylic acid esters of formula (I). n The β-ketocarboxylic acid esters readily accessible by the process according to the invention can be used as important intermediates in the synthesis of pharmaceutically active ingredients or plant protection agents.
专利号:US-5155251-A 优先权日:1991-10-11 标题:Process for the synthesis of (5R)-1,1-dimethylethyl-6-cyano-5-hydroxy-3-oxo-hexanoate 发明人:BUTLER DONALD E; LE TUNG V; MILLAR ALAN; NANNINGA THOMAS N 权利人:WARNER LAMBERT CO 摘要:An improved process for the preparation of (5R)-1,1-dimethylethyl-6-cyano-5-hydroxy-3-oxo-hexanoate is described where a halo hydroxyester or other activated dihydroxyester is converted in two steps to the desired product.
专利号:US-5248793-A 优先权日:1990-10-17 标 题:Process for the synthesis of (4R-cis)-1,1-dimethylethyl 6-iodomethyl or 6-(phenyl-substituted)sulfonyloxymethyl-2,2-dimethyl-1,3-dioxane-4-acetate 发明人:MILLAR ALAN; BUTLER DONALD E 权利人:WARNER LAMBERT CO 摘要:An improved process for the preparation of (4R-cis)-1,1-dimethylethyl 6-cyanomethyl-2,2-dimethyl-1,3-dioxane-4-acetate is described where a hydroxy ester derivative is converted in two steps to the desired product, as well as valuable intermediates used in the process.
摘要:Joule, J. A., Science of Synthesis Knowledge Updates, (2010) 2, 51. 摘要:Khartulyari, A.; Maier, M. E., Science of Synthesis Knowledge Updates, (2010) 3, 68. 摘要:Gao, W.-C.; Tian, J., Science of Synthesis Knowledge Updates, (2020) 3, 308. 摘要:Silva, V. L. M.; Pinto, D. C. G. A.; Santos, C. M. M.; Rocha, D. H. A., Science of Synthesis Knowledge Updates, (2022) 3, 195. 摘要:Sellars, J. D., Science of Synthesis Knowledge Updates, (2014) 1, 441.