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-2004058888-A1 优先权日:2000-01-13 标题:Methods for synthesis of alpha-d-gal (1~>3) gal-containing oligosaccharides 发明人:BORNAGHI LAURENT; DEKANY GYULA; DRINNAN NICHOLAS BARRY; PAPAGEORGIOU JOHN; WEST MICHAEL LEO 摘要:This invention relates to reagents and methods for synthesis of biologically active di- and tri-saccharides comprising α-D-Gal(1→3)-D-Gal. In particular the invention provides novel reagents, intermediates and processes for the solution or solid phase synthesis of α-D-galactopyranosyl-(1→3)-D-galactose, and derivatives thereof. In one preferred embodiments the invention provides a protected monosaccharide building block of general formula (II): in which R 3 is methoxy or methyl; R 1 is H, benzoyl, pivaloyl, 4-chlorobenzoyl, acetyl, chloroacetyl, levulinoyl, 4-methylbenzoyl, benzyl, 3,4-methylenedioxybenzyl, 4-methoxybenzyl, 4-chlorobenzyl, 4-acetamidobenzyl, or 4-azidobenzyl; and R 2 is H, Fmoc, benzoyl, pivaloyl, 4-chlorobenzoyl, acetyl, chloroacetyl, levulinoyl, 4-methylbenzoyl, benzyl, 3,4-methylenedioxybenzyl, 4-methoxybenzyl, 4 -chlorobenzyl, 4-acetamidobenzyl, or 4-azidobenzyl.
专利号:US-7102023-B2 优先权日:1999-11-24 标 题:Protecting groups useful in the synthesis of polysaccharides, natural products, and combinatorial libraries 发明人:BUCHWALD STEPHEN L; PLANTE OBADIAH J; SEEBERGER PETER H 权利人:MASSACHUSETTS INST TECHNOLOGY 摘要:One aspect of the present invention relates to optionally substituted halogenated benzyl halides and the like. These compounds are useful as halogenated benzyl ether-based protecting groups for a variety of functional groups. Another aspect of the present invention relates to use of said protecting groups in an orthogonal protecting group strategy for the synthesis of complex molecules that comprise a number of suitable functional groups. Another aspect of the present invention relates to saccharides bearing various arrays of protecting groups of the present invention. Another aspect of the present invention relates to a method of synthesizing an oligosaccharide or glycoconjugate, comprising the steps of: using a saccharide bearing at least one protecting group of the present invention to glycosylate a second molecule to give a product comprising said saccharide; and removing a protecting group of the present invention from said product.
专利号:EP-0791575-A1 优先权日:1996-02-16 标题 :Method of synthesis of a quaternary ammonium salt 发明人:NAKANO SHINJI 权利人:NIPPON PAINT CO LTD 摘要:The present invention provides an improved method of synthesis of a quaternary ammonium salt in which a tertiary amine is reacted with a benzyl halide optionally having on the benzene ring and/or at the α-site one ore more substituent groups inert to the reaction, which method is characterized in that the reaction is carried out in water or in a water-containing organic solvent.
专利号:US-6608202-B1 优先权日:2001-08-21 标题:Process of synthesis of a tricyclic ketone intermediate 发明人:DORAN HENRY J; O'NEILL PAT M; WILLIAMS ROBERT P 权利人:SCHERING CORP 摘要:In one embodiment, the present invention describes the synthesis of a compound of Formula III, wherein X is halogen,and intermediates therefor from easily available starting materials by a simple route.
专利号:US-7189864-B2 优先权日:1990-11-19 标 题:Method of preparing intermediates useful in synthesis of retroviral protease inhibitors 发明人:NG JOHN S; PRZYBYLA CLAIRE A; MUELLER RICHARD A; VAZQUEZ MICHAEL L; GETMAN DANIEL P 权利人:SEARLE & CO 摘要:A synthesis is described for intermediates which are readily amenable to the large scale preparation of hydroxyethylurea-based chiral HIV protease inhibitors. The method includes forming a diastereoselective epoxide from a chiral alpha amino aldehyde.
参考文献:10.1107/s1600536811015716 摘要:Keng TC, Lo KM, Ng SW. Bis{μ-2-[(N,N-diisopropylcarbamothioyl)sulfanyl]acetato-κ2O:O′}bis(bis(4-chlorobenzyl){2-[(N,N-diisopropylcarbamothioyl)sulfanyl]acetato-κ2O,O′}tin(IV)). Acta Crystallogr E Struct Rep Online. 2011 May 07;67(6):m661. doi: 10.1107/s1600536811015716. 参考文献:10.1107/s1600536811015728 摘要:Keng TC, Lo KM, Ng SW. Aquabis(4-chlorobenzyl)bis(nicotinato-κ2O,O′)tin(IV). Acta Crystallogr E Struct Rep Online. 2011 May 07;67(6):m662. doi: 10.1107/s1600536811015728. 参考文献:10.1107/s1600536811017156 摘要:Ge YQ, Zhang JM, Wang GL, Xu H, Shi B. Ethyl 1-(4-chloro-benz-yl)-3-(4-fluoro-phen-yl)-1H-pyrazole-5-carboxyl-ate. Acta Crystallogr Sect E Struct Rep Online. 2011 Jun 01;67(Pt 6):o1387.