专利号:US-6376649-B1 优先权日:1998-12-18 标题 :Methods for the synthesis of α- hydroxy-β-amino acid and amide derivatives 发明人:SEMPLE JOSEPH E; LEVY ODILE E 权利人:CORVAS INT INC 摘要:Methods for the synthesis of alpha-hydroxy-beta-amino acid and amide derivatives and alpha-ketoamide derivatives and novel derivatives made by these methods are provided. These methods involve reacting a N-terminally blocked (protected) aminoaldehyde with an isonitrile and a carboxylic acid to give an amino-alpha-acyloxy carboxamide. The acyloxy group may be removed to give the derivative. Alternatively the protecting group is removed and acyl shift occurs to give the derivative. These derivatives are useful in the synthesis of compounds such as peptidyl alpha-ketoamides and alpha-hydroxy-beta-carboxylic acid and amide derivatives. Certain of these compounds have been reported to have activity as inhibitors of proteases, such as serine proteases and cysteine proteases.
专利号:US-2024052391-A1 优先权日:2020-10-29 标 题 :Enzymatic Synthesis of Polynucleotide Probes 发明人:GODRON XAVIER; NIYOMCHON SUPAPORN; CHAMPION ELISE 权利人:DNA SCRIPT 摘要:The present invention is directed to methods and kits for enzymatic synthesis of labeled polynucleotide probes using template-free DNA polymerases.
专利号:US-2022411840-A1 优先权日:2019-11-13 标题 :High Efficiency Template-Free Enzymatic Synthesis of Polynucleotides 发明人:CHAMPION ELISE; SOSKINE MIKHAEL; SUNE ELODIE; YBERT THOMAS; GODRON XAVIER; HEINISCH TILLMANN 权利人:DNA SCRIPT 摘要:The invention is directed to compositions and methods for enzymatic template-free synthesis of polynucleotides wherein different terminal deoxynucleotidyl transferase (TdT) variants are used to incorporate different 3′-O-reversibly blocked deoxynucleoside triphosphates (dNTPs) into a growing chain. In part, the invention is a recognition and appreciation that different TdT variants can be engineered to preferentially incorporate specific dNTPs with higher efficiency than a single “general purposeâ€? TdT variant used to incorporate all four 3-O-reversibly blocked dNTPs.
专利号:US-6133409-A 优先权日:1996-12-19 标 题:Process for the solid phase synthesis of aldehyde, ketone, oxime, amine, hydroxamic acid and αβ-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 PHARM PROD INC 摘要:This invention is directed to a process for the solid phase synthesis of aldehyde, ketone, oxime, amine, hydroxamic acid and alpha , beta -unsaturated carboxylic acid and aldehyde compounds and to polymeric hydroxylamine resin compounds useful therefor.
专利号:US-8383810-B2 优先权日:2004-12-20 标题:Process for the synthesis of azetidinones 发明人:THIRUVENGADAM TIRUVETTIPURAM K; CHIU JOHN S; FU XIAOYONG; MCALLISTER TIMOTHY L 权利人:MERCK SHARP & DOHME; THIRUVENGADAM TIRUVETTIPURAM K; CHIU JOHN S; FU XIAOYONG; MCALLISTER TIMOTHY L 摘要:A process is provided for preparing azetidinones useful as intermediates in the synthesis of penems and as hypocholesterolemic agents, comprising reacting a β-(substituted-amino)amide, a β-(substituted-amino)acid ester, or a β-(substituted-amino)thiolcarbonic acid ester with a silylating agent and a cyclizing agent selected from the group consisting of alkali metal carboxylates, quaternary ammonium carboxylates, quaternary ammonium hydroxides, quaternary ammonium alkoxides, quaternary ammonium aryloxides and hydrates thereof, or the reaction product of: (i) at least one quaternary ammonium halide and at least one alkali metal carboxylate; or (ii) at least one quaternary ammonium chloride, quaternary ammonium bromide, or quaternary ammonium iodide and at least one alkali metal fluoride, wherein a quaternary ammonium moiety of the cyclizing agent is unsubstituted or substituted by one to four groups independently selected from the group consisting of alkyl, arylalkyl and arylalkyl-alkyl.
专利号:US-2017349928-A1 优先权日:2014-12-31 标 题:Methods for activating natural energy metabolism for improving yeast cell-free protein synthesis 发明人:JEWETT MICHAEL CHRISTOPHER; ANDERSON MARK J; STARK JESSICA CAROL; HODGMAN CHARLES ERIC 权利人:UNIV NORTHWESTERN 摘要:Disclosed are compositions, methods, and kits for enhanced synthesis of a biological macromolecule in vitro using cell-free protein synthesis. The compositions, methods, and kits include or utilize: a cell-free extract; a phosphate-free energy source; and a phosphate source, and typically do not include an exogenous nucleoside triphosphate or an exogenous nucleoside diphosphate.
[参考文献]: Luckose F, Et Al. Effects Of Amino Acid Derivatives On Physical, Mental, And Physiological Activities. Crit Rev Food Sci Nutr. 2015;55(13):1793-1144.
合成参考文献
参考文献:10.1055/s-0034-1380116 摘要:Grygorenko O, Ivon Y, Tymtsunik A, Komarov I, Shishkin O. Synthesis of a 2,5-Diazabicyclo[2.2.1]heptane-Derived α,β-Diamino Acid. Synthesis. 2015 Feb 03;47(08):1123–30. doi: 10.1055/s-0034-1380116.