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-2010099894-A1 优先权日:2006-10-09 标 题 :Method for the Synthesis of Cyclic Acetals by the Reactive Extraction of a Polyol in a Concentrated Solution 发明人:DUBOIS JEAN-LUC; IBORRA CHORNET SARA; VELTY ALEXANDRA I LUCIENNE; CORMA CANOS AVELINO 权利人:DUBOIS JEAN-LUC; IBORRA CHORNET SARA; VELTY ALEXANDRA I LUCIENNE; CORMA CANOS AVELINO 摘要:A method for the synthesis of cyclic acetals comprises reacting at least one carbonyl-function compound selected from aldehydes, ketones, and/or linear acetals, on a polyol in a concentrated aqueous solution exceeding 20 wt % in a reactor containing an acidic catalyst. The carbonyl-function compound is selected so that the cyclic acetal obtained has a water solubility lower than 20000 mg/kg. During the catalytic reaction for the cyclic acetal synthesis, at least one portion of the organic phase containing the cyclic acetal is separated. The acidic catalysis is either homogeneous when using a water-soluble strong acid, or heterogeneous when using a solid acid such as a resin, a zeolite, or any appropriately acidified solid. The extractive reaction method can be used for obtaining high conversions and selectivity.
专利号:US-11512303-B2 优先权日:2017-05-27 标 题 :Engineered polypeptides and their applications in the synthesis of beta-hydroxy-alpha-amino acids 发明人:CHEN HAIBIN; BONG YONG KOY; XU QING; ZHOU AMENG; SHEN TIANRAN; YANG JIADONG; YANG ZHUHONG 权利人:ENZYMASTER NINGBO BIO ENG CO LTD 摘要:The present invention provides engineered polypeptides that are useful for the asymmetric synthesis of β-hydroxy-α-amino acids under industrial-relevant conditions. The engineered polypeptides disclosed in this invention were developed through directed evolution based on the ability of catalytic synthesis of (2S, 3R)-2-amino-3-hydroxy-3-(4-nitrophenyl) propanoic acid. The present disclosure also provides polynucleotides encoding engineered polypeptides, host cells capable of expressing engineered polypeptides, and methods of producing β-hydroxy-α-amino acids using engineered polypeptides. Compared to other processes of preparation, the use of the engineered polypeptides of the present invention for the preparation of β-hydroxy-α-amino acids results in high purity of the desired stereoisomers, mild reaction conditions, low pollution and low energy consumption. So, it has good industrial application prospects.
专利号:US-3992439-A 优先权日:1972-04-17 标 题:Synthesis of prostaglandins of the 'one'-series 发明人:SCHAAF THOMAS K; COREY ELIAS J 权利人:PFIZER 摘要:In the synthesis of prostaglandins of the 'one' -series an alteration in the conventional reaction sequence avoids side reactions and provides an improved synthesis via a series of novel intermediates. In this improved synthesis the side chain at the 8 position is attached to the five membered ring before the side chain at the 12 position is attached.
专利号:US-5549974-A 优先权日:1994-06-23 标题:Methods for the solid phase synthesis of thiazolidinones, metathiazanones, and derivatives thereof 发明人:HOLMES CHRISTOPHER P 权利人:AFFYMAX TECH NV 摘要:The invention provides an efficient and versatile method for the combinatorial synthesis and screening of libraries of 4-thiazolidinones, metathiazanones, and derivatives thereof. In order to expediently synthesize a combinatorial library of derivatives based upon these core structures, a general methodology for the solid phase synthesis of these derivatives is also provided. Arrays of thiazolidinones, metathiazanones, and derivatives thereof useful as peptidomimetics and for the identification of agents having antifungal, antihistaminic, or antimicrobial activity or use in the treatment of inflammation, hypertension, renal failure, congestive heart failure, uremia and other conditions can be prepared using this method.
专利号:US-6512081-B1 优先权日:1997-07-21 标题:Synthesis of dithioester chain transfer agents and use of bis(thioacyl) disulfides or dithioesters as chain transfer agents 发明人:RIZZARDO ENZIO; THANG SAN HOA; MOAD GRAEME 权利人:E I DUPONT NEMOURS AND COMPANY; COMMW SCIENT IND RES ORG 摘要:This invention relates to the synthesis of dithiocarboxylic acid esters by reaction of bis(thioacyl) disulphides, thioacetals or vinylidane bis(thioether) with free-radicals (optionally in the presence of monomers). The invention also relates to processes for the synthesis of polymers utilising these dithioesters as polymerisation regulators (chain transfer agents) or to the use of bis(thioacyl) disulphides to generate dithioester chain transfer agents in situ.