专利号:US-5792892-A 优先权日:1994-04-28 标 题:Processes for preparing aromatic, bromine-containing compounds, novel bromine-containing compounds, and their use as intermediate products in the synthesis of active agents 发明人:HAGEMANN HERMANN 权利人:BAYER AG 摘要:The present invention relates to processes for the preparation of bromine-containing aromatic compounds, to novel bromine-containing compounds and to their use as intermediates in the synthesis of active substances. Processes according to the invention for the preparation of known and novel bromine-containing compounds are characterized by specific conditions.
专利号:US-7767826-B2 优先权日:2007-10-05 标题 :Process for the synthesis of L-(+)-ergothioneine 发明人:TRAMPOTA MIROSLAV 权利人:PHARMATECH INTERNATIONAL INC 摘要:This invention relates to a novel process for the preparation of optically pure L-(+)-ergothioneine. The process for the chemical synthesis of L-ergothioneine comprises steps which consist of reacting L-histidine alkyl ester with an acid halide, chloroformate or pyrocarbonate in the presence of a base, hydrolysis of the alkyl-(S,Z)-2,4,5-triamidopent-4-enoate to obtain a (S)-alkyl 2,5-diamido-4-oxopentanoate, acid catalyzed hydrolysis of the (S)-alkyl 2,5-diamido-4-oxopentanoate followed by reaction with a metal thiocyanate to obtain the thiohistidine, protection of the sulfur of thiohistidine as the tert-butyl thioether, dialkylation of the primary amine to obtain a tertiary amine, quaternization of the tertiary amine, and removal of the protecting group to obtain the desired (S)-3-(2-mercapto-1H-imidazol-5-yl)-2-(trialkylammonio)propanoate (I). This process affords a better yield and is capable of practical application at large scale.
专利号:US-6175009-B1 优先权日:1999-11-18 标题:Process for the preparation of quinazolinones 发明人:CONFALONE PASQUALE NICHOLAS; MAGNUS NICHOLAS ANDREW; STORACE LOUIS 权利人:DU PONT PHARM CO 摘要:The present invention relates generally to an asymmetric synthesis of 4,4-disubstituted-3,4-dihydro-2(1H)-quinazolinones, and intermediates thereof. The target compounds are useful for the treatment of human immunodeficiency virus (HIV) as an inhibitor of reverse transcriptase.
专利号:US-6022977-A 优先权日:1997-03-26 标 题 :Dynamic resolution of isoxazoline thioesters to isoxazoline carboxylic acids 发明人:ZHANG LIN-HUA; ANZALONE LUIGI; PESTI JAAN A; YIN JIANGUO 权利人:DU PONT PHARM CO 摘要:The present invention relates generally to a novel method for preparation of substituted isoxazolin-5-yl acetic acid in high optical purity from a stereoisomeric mixture of an esterified substituted isoxazolin-5-yl acetate. The products are useful in the synthesis of compounds for pharmaceuticals, especially the treatment of thrombolytic disorders, and agricultural products.
专利号:US-8129560-B2 优先权日:2005-08-15 标 题 :Process for the synthesis of mandipropamid and derivatives thereof 发明人:BOWDEN MARTIN CHARLES; CLARK THOMAS AITCHESON; GIORDANO FANNY; JAU BEAT; SCHNEIDER HANS-DIETER; SEIFERT GOTTFRIED; ZELLER MARTIN; FABER DOMINIK; WISS JUERG 权利人:BOWDEN MARTIN CHARLES; CLARK THOMAS AITCHESON; GIORDANO FANNY; JAU BEAT; SCHNEIDER HANS-DIETER; SEIFERT GOTTFRIED; ZELLER MARTIN; FABER DOMINIK; WISS JUERG; SYNGENTA CROP PROT INC 摘要:A process for the preparation of a compound of formula (I), the process comprising: (i) the reaction of a compound of formula (III), with a compound of formula (IV) to give a compound of formula (II), and (ii) the reaction of the compound of formula (II) with a leaving group, to give the compound of formula (I).
专利号:WO-0029391-A1 优先权日:1998-11-19 标题 :Process for the preparation of quinazolinones 发明人:CONFALONE PASQUALE NICHOLAS; MAGNUS NICHOLAS ANDREW; STORACE LOUIS 权利人:DU PONT PHARM CO 摘要:The present invention relates generally to an asymmetric synthesis of 4,4-disubstituted-3,4-dihydro-2(1H)-quinazolinones, and intermediates thereof. The target compounds are useful for the treatment of human immunodeficiency virus (HIV) as an inhibitor of reverse transcriptase.
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合成参考文献
摘要:Toxicology and Applied Pharmacology., 44(213), 1978 [] 摘要:Thomas JM et al; Ground Water 38: 605-14 (2000) 摘要:40 CFR 716.120 (USEPA); U.S. National Archives and Records Administration's Electronic Code of Federal Regulations. Available from, as of October 2, 2008: 摘要:USEPA/Office of Water; Federal-State Toxicology and Risk Analysis Committee (FSTRAC). Summary of State and Federal Drinking Water Standards and Guidelines (11/93) To Present 摘要:USEPA; Ambient Water Quality Criteria Doc: Halomethanes p.C-26 (1980) EPA 440/5-80-051