专利号:US-7589170-B1 优先权日:1998-09-25 标题 :Synthesis of cyclic peptides 发明人:SMYTHE MARK LESLIE; MEUTERMANS WIM DENIS FRANS; BOURNE GREGORY THOMAS; MCGEARY ROSS PETER 权利人:UNIV QUEENSLAND 摘要:This invention relates to methods for preparing cyclic peptides and peptidomimetic compounds in solution and bound to solid supports, and to cyclic peptide or peptidomimetic libraries for use in drug screening programs. In particular, the invention relates to a generic strategy for synthesis of cyclic peptides or peptidomimetics that enables the efficient synthesis under mild conditions of a wide variety of desired compounds. Two approaches were evaluated for their improvements in solution and solid phase synthesis of small cyclic peptides: positioning reversible N-amide substituents in the sequence; and applying native ligation chemistry in an intramolecular sense. Systematic investigation of the effects of preorganising peptides prior to cyclisation by using peptide cyclisation auxiliaries, and developing new linkers and peptide cyclisation auxiliaries to aid cyclic peptide synthesis gives surprising improvements in both yields and purity of products compared to the prior art methods. The combination of these technologies provides a powerful generic approach for the solution and solid phase synthesis of small cyclic peptides. The ring contraction and N-amide substitution technology of the invention provide improved methods for the synthesis of cyclic peptides and peptidomimetics. When used in conjunction with linker strategies, this combination provides solid-phase avenues to cyclic peptides and peptidomimetics.
专利号:US-6133018-A 优先权日:1997-06-02 标 题 :Enzymatic synthesis of chiral amines using -2-amino propane as amine donor 发明人:WU WEI; BHATIA MOHIT B; LEWIS CRAIG M; LANG WEI; WANG ALICE L; MATCHAM GEORGE W 权利人:CELGRO 摘要:2-Aminopropane is used as the amine donor in the stereoselective synthesis of a chiral amine from a ketone with a transaminase. In a typical embodiment, (S)-1-methoxy-2-aminopropane is prepared by bringing methoxyacetone into contact with a transaminase in the presence of 2-aminopropane as an amine donor until a substantial amount of methoxyacetone is converted to (S)-1-methoxy-2-aminopropane and 2-aminopropane is converted to acetone. In a second embodiment, L-alanine is prepared by bringing pyruvic acid into contact with a transaminase in the presence of 2-aminopropane as an amine donor.
专利号:US-7358382-B2 优先权日:2001-08-03 标 题 :Protected 3,5-dihydroxy-2,2-dimethyl-valeronitriles for the synthesis of epothilones and epothilone derivatives and process for the production 发明人:WESTERMANN JURGEN; PLATZEK JOHANNES; PETROV ORLIN 权利人:BAYER SCHERING PHARMA AG 摘要:The invention relates to 3,5-dihydroxy-2,2-dimethyl-valeronitriles for the synthesis of epothilones and epothilone derivatives and process for the production of these new intermediate products in the synthesis and the use for the production of epothilones or epothilone derivatives.
专利号:US-7368568-B2 优先权日:2001-08-03 标 题 :Protected 3,5-dihydroxy-2,2-dimethyl-valeroamides for the synthesis of epothilones and derivatives and process for production and the use 发明人:WESTERMANN JURGEN; PLATZEK JOHANNES; PETROV ORLIN 权利人:BAYER SCHERING PHARMA AG 摘要:The invention relates to new protected 3,5-dihydroxy-2,2-dimethyl-valeroarnides for the synthesis of edothilones and derivatives and process for the production and the use of the new compounds for the production of epothilones or epothilone derivatives.
专利号:US-10023677-B2 优先权日:2014-12-16 标 题 :Method for controlling the synthesis of a block copolymer containing at least one nonpolar block and at least one polar block and use of said block copolymer in applications of nanolithography by direct self-assembly 发明人:NAVARRO CHRISTOPHE; NICOLET CELIA; CHEVALIER XAVIER 权利人:ARKEMA FRANCE 摘要:A method for controlling the synthesis of a block copolymer containing at least two blocks, with at least one nonpolar block and at least one polar block, said method making it possible in particular to control the ratio between the blocks and the molecular weight of each of the blocks, said copolymer being a block copolymer intended to be used as a mask in a method of nanolithography by direct self-assembly (DSA), said control being achieved by semicontinuous anionic polymerization in an aprotic nonpolar medium.
专利号:US-10280189-B2 优先权日:2012-07-17 标题:Method for the synthesis of aminoalkylenephosphonic acid 发明人:BURCK SEBASTIAN; LECLERCQ CEDRIC NICOLAS; NOTTE PATRICK 权利人:MONSANTO TECHNOLOGY LLC 摘要:A method for the synthesis of an aminoalkylenephosphonic acid or its phosphonate esters including the following steps: a) forming, in the presence of an aldehyde or ketone and an acid catalyst, a reaction mixture by mixing a compound having at least one HNR 1 R 2 moiety or a salt thereof, with a compound having one or more P—O—P anhydride moieties, the moieties having one P atom at the oxidation state (+III) and one P atom at the oxidation state (+III) or (+V), wherein the ratio of moles of aldehyde or ketone to N—H moieties is 1 or more and wherein the ratio of N—H moieties to P—O—P anhydride moieties is 0.3 or more, and b) recovering the resulting aminoalkylenephosphonic acid having compound or its phosphonate esters.
参考标题:Rapid And Quantitative Profiling Of Substrate Specificity Of ω‐transaminases For Ketones 作者:Sang‐woo Han,Jong‐shik Shin |发布日期:2019.7.18 摘要:Capability For Asymmetric Synthesis Of Chiral Amines From Ketones. Reliable High‐throughput Activity Assay Of ω‐tas Is Essential In Carrying Out Extensive Substrate Profiling And Establishing A Robust Screening Platform. Here We Report Spectrophotometric And Colorimetric Methods Enabling Rapid Quantitation Of ω‐ta Activities Toward Ketones In A 96‐well Microplate Format. The Assay Methods Employ Benzylamine
合成参考文献
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