专利号:US-12240808-B2 优先权日:2021-05-28 标 题 :Process for the synthesis of calebin-a and its intermediates 发明人:MAJEED MUHAMMED; NAGABHUSHANAM KALYANAM; MUTHUKAMAN NAGARAJAN; NAIDU PENTAKOTA PARADESI 权利人:MAJEED MUHAMMED; NAGABHUSHANAM KALYANAM; MUTHUKAMAN NAGARAJAN; NAIDU PENTAKOTA PARADESI 摘要:The invention discloses novel intermediates in the synthesis of Calebin A represented by formula 3. The invention also covers processes for the synthesis of Calebin-A and its analogs using compounds of formula 3.
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-4190579-A 优先权日:1977-12-29 标题:Synthesis of beta-lactams from azetidine carboxylic acid esters 发明人:LIPSHUTZ BRUCE H; WASSERMAN HARRY H; WU JAMES S 权利人:RESEARCH CORP 摘要:Azetidine carboxylic acid esters are converted into enol silyl ethers which, as enamino ketene acetals, undergo ready oxidative cleavage of the ethylenically unsaturated double bond, e.g. by dye-sensitized photo-oxygenation, to form beta-lactams. The beta-lactams and substitution products thereof are useful intermediates in the synthesis of biologically active lactams.
专利号:US-4110380-A 优先权日:1974-05-06 标题 :Asymmetric synthesis of organic compounds 发明人:HAJOS ZOLTAN GEORGE; PARRISH DAVID RICHARD 权利人:HOFFMANN LA ROCHE 摘要:Optically active organic compounds are prepared starting from optically inactive reactants by means of an optically active agent which influences the course of the reaction. In particular optically active compounds having a 'meso' type carbon atom undergo an intramolecular ring closure in the presence of an optically active agent to yield an optically active product having one additional ring. The present process is particularly useful in the preparation of optically active bicyclic diketones which are important intermediates in the total synthesis of steroids.
专利号:US-9206222-B2 优先权日:2009-06-29 标题:Solid phase peptide synthesis of peptide alcohols 发明人:CAUSSIL-AMBLARD MURIEL; MARTINEZ JEAN; TAILHADES JULIEN 权利人:CAUSSIL-AMBLARD MURIEL; MARTINEZ JEAN; TAILHADES JULIEN; CENTRE NAT RECH SCIENT 摘要:The present invention relates to the synthesis of depsipeptides on solid phase support. Said depsipeptides are then implicated in a solution phase O—N acyl shift enabling to obtain the corresponding peptide alcohols.
专利号:US-2003180804-A1 优先权日:2001-10-29 标题:Solid phase synthesis of chemical libraries 发明人:PRYOR KENT E; LEWIS RONALD D; BROWN JASON W 权利人:CORVAS INT INC 摘要:The present invention provides compounds and compound libraries that are useful as protease modulators. The compounds and compound libraries are preferably made using the methods of the present invention which utilize peptide synthesis and combinatorial chemistry methods on a solid phase.
1: Sato T, Hoshida H, Akada R. Inhibition of Distinct Proline- or N-Acetylglucosamine-Induced Hyphal Formation Pathways by Proline Analogs in Candida albicans. Biomed Res Int. 2020 Nov 17;2020:7245782. doi: 10.1155/2020/7245782. 2: Berg MD, Zhu Y, Isaacson J, Genereaux J, Loll-Krippleber R, Brown GW, Brandl CJ. Chemical-Genetic Interactions with the Proline Analog L-Azetidine-2-Carboxylic Acid in Saccharomyces cerevisiae. G3 (Bethesda). 2020 Dec 3;10(12):4335-4345. doi: 10.1534/g3.120.401876. 3: Mat Nanyan NSB, Watanabe D, Sugimoto Y, Takagi H. Involvement of the stress- responsive transcription factor gene MSN2 in the control of amino acid uptake in Saccharomyces cerevisiae. FEMS Yeast Res. 2019 Aug 1;19(5):foz052. doi: 10.1093/femsyr/foz052. 51(8):1221-1232. doi: 10.1007/s00726-019-02763-w. Epub 2019 Jul 13. 7(12):239. doi: 10.3390/cells7120239.
合成参考文献
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