专利号:US-6710208-B2 优先权日:1996-12-19 标题 :Process for the solid phase synthesis of aldehyde, ketone, oxime, amine, hydroxamic acid and α,β-unsaturated carboxylic acid and aldehyde compounds 发明人:SALVINO JOSEPH M; MORTON GEORGE C; MASON HELEN J; LABAUDINIERE RICHARD F 权利人:AVENTIS PHARMA INC 摘要:This invention is directed to a process for the solid phase synthesis of aldehyde, ketone, oxime, amine, hydroxamic acid and α,β-unsaturated carboxylic acid and aldehyde compounds and to polymeric hydroxylamine resin compounds useful therefor.
专利号:WO-2008150031-A1 优先权日:2007-06-08 标题:Inhibitor of biosynthesis of plant hormone auxin, chemical plant regulator comprising the inhibitor as active ingredient, herbicidal agent, and use thereof 发明人:SHIMADA YUKIHISA; GODA HIDEKI; TACHIKAWA TOMOE; ISHII TAKAHIRO; SOENO KAZUO; FUJIOKA SHOZO; ASAMI TADAO 权利人:RIKEN; SHIMADA YUKIHISA; GODA HIDEKI; TACHIKAWA TOMOE; ISHII TAKAHIRO; SOENO KAZUO; FUJIOKA SHOZO; ASAMI TADAO 摘要:The first object is to provide an inhibitor of the synthesis of endogenous auxin. The second object is to provide a plant growth inhibitor or a herbicidal agent utilizing the auxin biosynthesis inhibitor. Thus, disclosed are: a method for screening a candidate for an auxin biosynthesis inhibitor capable of inhibiting the expression of an auxin-inducible gene, by adding each of candidate compounds for the auxin inhibitor to a plant; a method for selecting a compound capable of actually inhibiting the auxin synthesis in a plant, by adding each of candidate compounds to the plant, disrupting the plant and then measuring the amount of endogenous auxin; and a method for selecting a compound capable of inhibiting the production of indolpyruvic acid in the presence of a tryptophan deaminase and tryptophan which are prepared in advance. More specifically disclosed are: an auxin biosynthesis inhibitor comprising AVG, AOA, AOIBA, L-AOPP or an analogue thereof; and a plant growth regulator or a herbicidal agent comprising the compound as an active ingredient.
专利号:US-6093812-A 优先权日:1991-07-23 标 题 :Process for the stereospecific synthesis of azetidinones 发明人:THIRUVENGADAM TIRUVETTIPURAM K; TANN CHOU-HONG; LEE JUNNING; MCALLISTER TIMOTHY; COLON CESAR; BARTON DEREK H R; BRESLOW RONALD; SUDHAKAR ANANTHA 权利人:SCHERING CORP 摘要:This invention provides an improved process for producing azetidinones. More particularly, this invention provides the steps of producing an trans-azetidinone represented by the formula from a carboxylic acid R2-D-CH2COOH, an aldehyde R1-A-CHO and an amine RNH2, by the steps of: (a1) converting a carboxylic acid to the corresponding acid chloride; (b1) deprotonating a chiral oxazolidinone and treating the resulting anion with the product of step (a1); (c1) enolizing the product of step (b1) and condensing with the aldehyde; (d1) hydrolyzing the product of step (c1); (e1) condensing the product of step (d1) with the amine; and (f1) cyclizing the product of step (e1). Alternatively, the process comprises (a2) enolizing the product of step (b1) and condensing, in the presence of a Lewis acid, with a Schiff's base prepared from the aldehyde and the amine; and (b2) cyclizing the product of step (a2).
专利号:US-6180830-B1 优先权日:1995-11-08 标题 :Method for preparing a bimetallic ruthenium/tin catalyst and a process for the synthesis of aldehydes 发明人:JACQUOT ROLAND 权利人:RHODIA CHIMIE SA 摘要:The present invention relates to a new process for the preparation of a bimetallic ruthenium/tin catalyst. The process for the preparation of a bimetallic ruthenium/tin catalyst according to the invention is characterised by the fact that it consists in carrying out the reduction of a ruthenium complex having an electrovalency of -4 and a coordination number of 6, the ligands being either a halogen atom or an anion or a tin halide. The catalyst is further employed for the preparation of aldehydes by reduction, in the vapor phase, of carboxylic acids, esters and anhydrides.
专利号:US-8017776-B2 优先权日:2003-07-15 标题 :Methods for synthesis of acyloxyalkyl compounds 发明人:BHAT LAXMINARAYAN; GALLOP MARK A 权利人:XENOPORT INC 摘要:Disclosed herein are methods for synthesizing 1-(acyloxy)-alkyl prodrug derivatives of drugs through oxidation of 1-acyl-alkyl derivatives of drugs under anhydrous reaction conditions. The methods typically proceed stereospecifically, in high yield, do not require the use of activated intermediates and/or toxic compounds and are readily amenable to scale-up.
专利号:US-5561227-A 优先权日:1991-07-23 标题:Process for the stereospecific synthesis of azetidinones 发明人:THIRUVENGADAM TIRUVETTIPURAM K; TANN CHOU-HONG; MCALLISTER TIMOTHY L 权利人:SCHERING CORP 摘要:This invention provides an improved process for producing azetidinones. More particularly, this invention provides the steps of producing an azetidinone represented by the formula I ##STR1## from a carboxylic acid R 2 --D--CH 2 COOH, an aldehyde R 1 --A--CHO and an amine RNH 2 , by the steps of: (a) converting a carboxylic acid to the corresponding acid chloride; (b) deprotonating a chiral oxazolidinone and treating the resulting anion with the product of step (a); (c) enolizing the product of step (b) and condensing with an imine; and (d) cyclizing the product of step (c). Steps (c) and (d) of this process are as shown in the following reaction scheme. ##STR2##
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