专利号:US-8153839-B2 优先权日:2005-09-14 标题:Method for synthesis of keto acids or amino acids by hydration of acetylene compound 发明人:OGO SEIJI; FUKUZUMI SHUN-ICHI 权利人:OGO SEIJI; FUKUZUMI SHUN-ICHI; JAPAN SCIENCE & TECH AGENCY 摘要:An object of the present invention is to provide a method for synthesis of keto acids by hydration of an acetylene compound (acetylene-carboxylic acids) under mild conditions free from harmful mercury catalysts and a method for synthesis of amino acids from acetylene-carboxylic acids in a single container (one-pot or tandem synthesis). In one embodiment of the method according to the present invention for synthesis of keto acids, acetylene-carboxylic acids is hydrated in the presence of a metal salt represented by General Formula (1), n nwhere M 1 represents an element in Group VIII, IX, or X of the periodic table, and X 1 , X 2 , or X 3 ligand represents halogen, H 2 O, or a solvent molecule, and k represents a valence of a cation species, and Y represents an anion species, and L represents a valence of the anion species, and each of K and L independently represents 1 or 2, and k×m=L×n.
专利号:US-9376461-B2 优先权日:2011-06-06 标 题:Non-enzymatic synthesis of O-acetyl-ADP-ribose and analogues thereof 发明人:KOPPETSCH KARSTEN; SZCZEPANKIEWICZ BRUCE G; PERNI ROBERT B 权利人:KOPPETSCH KARSTEN; SZCZEPANKIEWICZ BRUCE G; PERNI ROBERT B; GLAXOSMITHKLINE LLC 摘要:Provided herein is a simple, one-step, non-enzymatic synthesis of O-Acetyl-ADP-ribose (OAADPR) from NAD and sodium acetate in acetic acid. The extension of this reaction to other carboxylic acids, demonstrates that the reaction between NAD, and NAD analogs produces mixtures of the corresponding 2′- and 3′-carboxylic esters. Included are O-carboxyl-ADP-ribose compounds and corresponding methods of synthesis (e.g., O-propionyl-ADP-ribose, O-succinyl-ADP-ribose, O-malonyl-ADP-ribose), as well as non-adenosine nucleoside compounds.
专利号:US-2023286918-A1 优先权日:2020-07-02 标 题:Manufacturing process for 3,5-dichloropicolinonitrile for synthesis of vadadustat 发明人:JURKAUSKAS VALDAS; JUNG YOUNG CHUN; KWON TAESOO; KANNAN ARUNACHALAM; GONDI VIJAYA BHASKER 权利人:AKEBIA THERAPEUTICS INC 摘要:Disclosed herein are methods and processes of preparing vadadustat or a pharmaceutically acceptable salts thereof, and intermediates (e.g., a compound of Formula (I), (I-F), (II), or (IV), or a pharmaceutically acceptable salts thereof) useful for the synthesis of vadadustat.
专利号:US-8697876-B2 优先权日:2010-04-02 标 题:Compositions and methods of synthesis of pyridinolypiperidine 5-HT1F agonists 发明人:CARNIAUX JEAN-FRANCOIS; CUMMINS JONATHAN 权利人:CARNIAUX JEAN-FRANCOIS; CUMMINS JONATHAN; COLUCID PHARMACEUTICALS INC 摘要:The present invention provides a novel polymorph of the hemisuccinate salt of 2,4,6-trifluoro-N-[6-(1-methyl-piperidine-4-carbonyl)-pyridin-2-yl]-benzamide (Form A) characterized by a unique X-ray diffraction pattern and Differential Scanning Calorimetry profile, as well as a unique crystalline structure. This polymorph is useful in pharmaceutical compositions, for example, for the treatment and prevention of migraine. The invention also provides a process for the synthesis of pyridinoylpiperidine compounds of Formula I in high yield and high purity. In particular, the provides a process for the preparation of 2,4,6-trifluoro-N-[6-(1-methyl-piperidine-4-carbonyl)-pyridin-2-yl]-benzamide, its hemisuccinate salt and polymorph (Form A).
专利号:US-9000209-B2 优先权日:2011-07-22 标题:Method of regioselective synthesis of substituted benzoates 发明人:KRAUS GEORGE A 权利人:KRAUS GEORGE A; UNIV IOWA STATE RES FOUND INC 摘要:A method of synthesis of para-substituted benzoate esters and acids is provided, wherein the para-substituted regioisomer is obtained substantially free of the meta-substituted impurity, the method comprising contacting a coumalate ester or acid and an unactivated alkene at elevated temperature in the presence of a metal oxidation catalyst and an oxidant. The metal oxidation catalyst can be palladium, such as palladium on carbon, and the oxidant can be the oxygen gas in ambient air. The reaction can be carried out without solvent or in high boiling hydrocarbon solvents such as mesitylene. When the unactivated alkene is a monosubstituted alkene, yields of at least about 50 or 60% of para-substituted ester and acid products, respectively, are obtained, substantially free of the regioisomeric meta-substituted impurity.
专利号:US-11414375-B2 优先权日:2016-07-29 标题:Mild and efficient preparation method for α-acyloxyenamide compounds and use thereof in synthesis of amide and polypeptide 发明人:ZHAO JUNFENG; HU LONG; XU SILIN; ZHAO ZHENGUANG 权利人:UNIV JIANGXI NORMAL 摘要:Disclosed are a mild and efficient preparation method for an α-acyloxyenamide compound and a use thereof in the synthesis of an amide and a polypeptide. The α-acyloxyenamide compound is obtained by an addition reaction of a ynamide and a carboxylic acid in dichloromethane under conditions where the temperature is 0° C. to 50° C.; the produced α-acyloxyenamide compound can react with an amine compound to produce an amide or a polypeptide; the two reactions can be carried out step by step, and can also be carried out in one pot. According to the invention, the reaction conditions are mild and no metal catalyst is required; when the carboxylic acid, which has chirality on an alpha site of carboxyl, forms an amide bond or a peptide bond, no racemization occurs; and the operation is simple and the application range is wide.