专利号:US-8350031-B2 优先权日:2008-06-02 标 题:Processes for the synthesis of levocetirizine and intermediates for use therein 发明人:RAO DHARMARAJ RAMACHANDRA; KANKAN RAJENDRA NARAYANRAO; GHAGARE MARUTI; CHIKHALIKAR SANDIP VASANT 权利人:CIPLA LTD; RAO DHARMARAJ RAMACHANDRA; KANKAN RAJENDRA NARAYANRAO; GHAGARE MARUTI; CHIKHALIKAR SANDIP VASANT 摘要:The present invention provides a compound of formula (IV) n nwherein R is Cl, Br, NO 2 , OH or OR′, and R′ is alkyl, and its use in the synthesis of levocetirizine, including its use in the synthesis of (−)-1-[(4-chlorophenyl)-phenylmethyl]piperazine, an intermediate useful in the synthesis of levocetirizine. The present invention also provides compounds (II) and (III) which are useful in the synthesis of compound (IV).
专利号:US-4210598-A 优先权日:1977-02-25 标 题 :Process for the industrial synthesis of vinyl and isopropenyl chloroformate and thiochloroformate 发明人:MALFROOT THIERRY A; PITEAU MARC D 权利人:POUDRES & EXPLOSIFS STE NALE 摘要:The invention relates to a process for the industrial scale synthesis of vinyl and isopropenyl chloroformates and thiochloroformates. According to the invention, phosgene or thiophosgene is reacted, at between 20 DEG and 70 DEG C., with a mercury salt XHg(CH2CRO), in which X=Cl or -CH2CRO, where R=H or CH3, in the presence of a solvent or a mixture of solvents having a dielectric constant greater than 10. The process can also be carried out using a mixture of the above solvents with a solvent which is not effective by itself (solvent of low polarity) but which is inexpensive. The yields achieved can exceed 90%.
专利号:US-8106201-B2 优先权日:2003-09-22 标 题:Process for the synthesis of morphinane compounds and intermediates thereof 发明人:SMITH CRAIG; PURCELL STUART; WADDELL LUCY; HAYES NICHOLAS; RITCHIE JARROD; HALLIDAY SCOTT BRIAN; MITCHELL MELVILLE; WILSON GEORGE SCOTT 权利人:SMITH CRAIG; PURCELL STUART; WADDELL LUCY; HAYES NICHOLAS; RITCHIE JARROD; HALLIDAY SCOTT BRIAN; MITCHELL MELVILLE; WILSON GEORGE SCOTT; JOHNSON MATTHEY PLC; GLAXOSMITHKLINE AUSTRALIA PTY LTD 摘要:This invention relates to intermediates useful in the preparation of opiate alkaloids, particularly morphinane compounds. The invention also relates to processes for preparing such intermediates and to processes which utilise such intermediates in the synthesis of morphinane compounds.
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-9546161-B2 优先权日:2001-07-16 标题:Synthesis of UDP-glucose: N-acylsphingosine glucosyl transferase inhibitors 发明人:HIRTH BRADFORD H; SIEGEL CRAIG 权利人:GENZYME CORP 摘要:Disclosed is a novel enantiomeric synthesis ceramide-like inhibitors of UDP-glucose: N-acylsphingosine glucosyltransferase. Also disclosed are novel intermediates formed during the synthesis.
专利号:EP-1892237-A1 优先权日:2004-01-28 标 题 :Vinylchloroformate-free synthesis of vinyl and allyl(thio)carbamates 发明人:SEELYE DAVID E; KUNZLER JAY F; SALAMONE JOSEPH C 权利人:BAUSCH & LOMB 摘要:The invention generally relates to methods of forming allyl(thio)carbamates and more particularly to a method of synthesizing allyl(thio)carbamates that does not necessitate the use of phosgene and organomercury intermediates.