专利号:US-8436206-B2 优先权日:2007-08-03 标 题:Process for the synthesis of (7-methoxy-1-naphthyl) acetonitrile and application in the synthesis of agomelatine 发明人:DUBUFFET THIERRY; LECOUVE JEAN-PIERRE; HERMET JEAN-PAUL 权利人:DUBUFFET THIERRY; LECOUVE JEAN-PIERRE; HERMET JEAN-PAUL; SERVIER LAB 摘要:Process for the industrial synthesis of the compound of formula (I) n nApplication of such process in the synthesis of agomelatine.
专利号:US-2006167289-A1 优先权日:2003-12-05 标题 :Practical, cost-effective synthesis of ubiquinones 发明人:LIPSHUTZ BRUCE H; BERL VOLKER; SCHEIN KARIN; WETTERICH FRANK 权利人:ZYMES LLC 摘要:The present invention provides a convergent method for the synthesis of ubiquinones and ubiquinone analogues. Also provided are precursors of ubiquinones and their analogues that are useful in the methods of the invention. The invention further provides an improved method for the carboalumination of alkyne substrates.
专利号:US-9085518-B2 优先权日:2011-10-14 标题 :Method for the synthesis of 18F-labelled molecules 发明人:NAIRNE ROBERT JAMES DOMETT; BHALLA RAJIV; KHAN IMTIAZ; BROWN JANE; WILSON ANTHONY; BLACK ANDRES 权利人:GE HEALTHCARE LTD 摘要:The present invention provides a method for the synthesis of 18F-labelled biomolecules, which is amenable to automation. The present invention also provides a cassette for automating the method of the invention. The method of the present invention provides numerous advantages over the prior art methods. One less purification step is required as compared with known methods. Also, in a preferred embodiment, one less reagent is required as a particular reagent is employed in two different steps. The chemistry process is thereby simplified, the cost of goods is reduced and the burden of validation and documentation of reagents required for GMP clinical production is minimized.
专利号:US-8492390-B2 优先权日:2002-05-08 标题 :Synthesis of locked nucleic acid derivatives 发明人:DETLEF SORENSEN MADS; WENGEL JESPER; KOCH TROELS; CHRISTENSEN SIGNE M; ROSENBOHM CHRISTOPH; PEDERSEN DANIEL SEJER 权利人:DETLEF SORENSEN MADS; WENGEL JESPER; KOCH TROELS; CHRISTENSEN SIGNE M; ROSENBOHM CHRISTOPH; PEDERSEN DANIEL SEJER; SANTARIS PHARMA AS 摘要:The invention relates to a novel strategy for the synthesis of Locked Nucleic Acid derivatives, such as α- L -oxy-LNA, amino-LNA, α- L -amino-LNA, thio-LNA, α- L -thio-LNA, seleno-LNA and methylene LNA, which provides scalable high yielding reactions utilising intermediates that also can produce other LNA analogues such as oxy-LNA. Also, the compounds of the formula X are important intermediates that may be reacted with varieties of nucleophiles leading to a wide variety of LNA analogues.
专利号:US-5326885-A 优先权日:1992-05-01 标 题 :Process of preparing enriched enantiomers of glycerol carbonate and derivatives thereof for synthesis of β-blockers 发明人:OLIVERO ALAN G; CASSEL JONATHAN M; POULSEN JAMES R 权利人:COGNIS INC 摘要:Enriched enantiomers of glycerol Carbonate are produced under the influence of a hydrolytic enzyme, either by selective esterification of racemic glycerol carbonate or by selective hydrolysis of an ester of the racemate. The enriched enantiomeric product is readily converted to starting materials and intermediates useful in the synthesis of enantiomerically pure therapeutic agents, such as beta -adrenergic blockers.
专利号:US-6700001-B2 优先权日:2001-10-05 标 题:Process for stereoselective synthesis of 2-hydroxymethyl chromans 发明人:GROSS JONATHAN L; STACK GARY P 权利人:WYETH CORP 摘要:A process for the stereoselective synthesis of 2-hydroxymethyl-chromans of formula (II) is providedwhere R, R<1>, R<2 >and R<3 >are as defined herein. The compound of formula (II) is prepared using an optically active benzene compound of formula (I)where R<0 >is as defined herein. The 2-hydroxymethyl-chroman compounds of formula (II) are useful as intermediates for preparing a variety of medicinal agents.