专利号:US-6013829-A 优先权日:1996-02-05 标 题 :Process for the asymmetric synthesis of S-acyl derivatives of 2-mercaptomethyl -3- phenyl propanoic acid, application to the synthesis of N-(mercaptoacyl) amino acid derivatives 发明人:DANVY DENIS; MONTEIL THIERRY; DUHAMEL PIERRE; DUHAMEL LUCETTE; LECOMTE JEANNE-MARIE; SCHWARTZ JEAN-CHARLES; NOEL-LEFEBVRE NADINE; GROS CLAUDE; PLAQUEVENT JEAN-CHRISTOPHE 权利人:BIOPROJET SOC CIV 摘要:PCT No. PCT/FR97/00218 Sec. 371 Date Nov. 26, 1997 Sec. 102(e) Date Nov. 26, 1997 PCT Filed Feb. 4, 1997 PCT Pub. No. WO97/29086 PCT Pub. Date Aug. 14, 1997Process for the asymmetric synthesis of S-acyl derivatives of 2-mercaptomethyl-3-phenylpropanoic acid of formula (I): characterized in that it comprises the steps consisting in: a) preparing the diol (VI) by reduction of a malonic ester (V) in the presence of a hydride; b) preparing the monoacetates (VII R) or (VII S) respectively; c) subjecting these monoacetates to an oxidation in order to form the acids (IX S) or (IX R); d) saponifying the compounds (IX S) or (IX R) in order to form the hydroxy acids (X S) or (X R); e) thioacylating the hydroxy acids (X S) or (X R) with a mercapto acid R1SH (XI), according to a Mitsunobu-type reaction, in order to lead to the desired acids (I R) (I S) respectively and application to the synthesis of N-(mercaptoacyl)amino acid derivatives (II).
专利号:US-4288608-A 优先权日:1978-06-01 标题:Synthesis of anthracyclines 发明人:JOHNSON FRANCIS; KIM KYOUNG S 权利人:RESEARCH CORP 摘要:There is provided a novel method of synthesizing certain heterocyclic quinones. In particular there is provided a novel and regiospecific synthesis of 9-acetyl-6,11-dihydroxy-4-methoxy-7,8,9,10-tetrahydronaphthacene-5,12-quinone (7,9-dideoxydaunomycinone) which is known intermediate in the synthesis of daunomycinone. There is also provided a method of preparing analogs of 7,9-dideoxydaunomycinone which thus provide for the preparation of known and desired analogs of daunomycinone. Daunomycinone is a known compound which is an intermediate in the preparation of the clinically accepted naturally-occurring antitumor antibiotics daunomycin and its derivitive adriamycin.
专利号:US-5945548-A 优先权日:1995-03-03 标题:Process for the synthesis of α-substituted acrylic acids and their application 发明人:DUHAMEL PIERRE; DUHAMEL LUCETTE; DANVY DENIS; MONTEIL THIERRY; LECOMTE JEANNE-MARIE; SCHWARTZ JEAN-CHARLES 权利人:BIOPROJECT SOC CIV 摘要:Process for the synthesis of α-substituted acrylic acids of general formula (I) and their application to the synthesis of N-(mercaptoacyl)aminoacid derivatives of formula (II). ##STR1##
专利号:US-4870207-A 优先权日:1983-06-17 标题 :Synthesis of arphamenine A 发明人:UMEZAWA HAMAO; AOYAGI TAKAAKI; TATSUTA KUNIAKI; NAKAMURA TAKESHI; FUKATSU SHUNZO 权利人:MICROBIAL CHEM RES FOUND 摘要:Known compound, optically active arphamenine A can now be synthesized in an optically active pure form and in a favorable yield by a new process comprising consecutive steps with starting from L-arginine, wherein racemization of intermediate reaction products can be minimized.
专利号:US-7060818-B2 优先权日:2003-02-21 标题:Synthesis of macrocyclic tetraamido compounds and new metal insertion process 发明人:HORWITZ COLIN P; GHOSH ANINDYA 权利人:UNIV CARNEGIE MELLON 摘要:An improved method of synthesizing a macrocyclic tetraamido compound includes protecting the amino portion of an amino carboxylic acid to form a protected amino carboxylic acid; exposing the protected amino carboxylic acid to a first solvent, preferably a hydrocarbon solvent, such as toluene or 1,2-dichloroethane, dichloromethane, dibromomethane and 1,2-dibromoethane. The carboxylic acid portion of the protected amino carboxylic acid is then converted to an activated carboxylic acid by one of esterification or acid halide formation, to form a protected amino activated carboxylic acid derivative. The protected amino activated carboxylic acid derivative is reacted with a diamine in the presence of a second solvent, such as THF or ,2-dichloroethane, dichloromethane, dibromomethane and 1,2-dibromoethane, to form a protected diamide diamine intermediate. Following deprotection, the diamide diamine intermediate is reacted with an activated diacid, such as an activated malonate, oxalate or succinate derivative to form the macrocyclic tetraamido compound. The macrocyclic tetraamido compound may further be complexed with a transition metal.
专利号:US-2009111737-A1 优先权日:1999-05-24 标题:Novel antibacterial agents 发明人:CHRISTENSEN BURTON G; MORAN EDMUND J; GRIFFIN JOHN H; JUDICE J KEVIN; MU YONGQI; PACE JOHN L; MAMMEN MATHAI; AGGEN JAMES 权利人:CHRISTENSEN BURTON G; MORAN EDMUND J; GRIFFIN JOHN H; JUDICE J KEVIN; MU YONGQI; PACE JOHN L; MAMMEN MATHAI; AGGEN JAMES 摘要:This invention relates to novel multibinding compounds (agents) that are antibacterial agents. The multibinding compounds of the invention comprise from 2-10 ligands covalently connected by a linker or linkers, wherein each of said ligands in their monovalent (i.e., unlinked) state have the ability to bind to a an enzyme involved in cell wall biosynthesis and metabolism, a precursor used in the synthesis of the bacterial cell wall and/or the bacterial cell surface thereby interfere with the synthesis and/or metabolism of the cell wall. In particular the multibinding compounds of the invention comprise from 2-10 ligands covalently connected by a linker or linkers, wherein each of said ligands hasn a ligand domain capable of binding to penicillin binding proteins, a transpeptidase enzyme, a substrate of a transpeptidase enzyme, a beta-lactamase enzyme, pencillinase enzyme, cephalosporinase enzyme, a transglycoslase enzyme, or a transglycosylase enzyme substrate; Preferably, the ligands are selected from the beta lactam or glycopeptide class of antibacterial agents.
摘要:T. C. Kawassisales, T. A. Kouimtzis and J. A. Tossidis, Chim. Chron., A 33, 1 (1968); CA 69, 5686n. 摘要:V. S. K. Nair and S. Parthasarathy, J. Inorg. Nucl. Chem. 32, 3289 (1970).