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-11479577-B2 优先权日:2016-05-18 标题:Intermediates for the synthesis of bile acid derivatives, in particular of obeticholic acid 发明人:WEYMOUTH-WILSON ALEXANDER; KOMSTA ZOFIA; WALLIS LAURA; EVANS TIMOTHY; DAVIES IEUAN; OTTER CARL; BATCHELOR RHYS 权利人:NZP UK LTD 摘要:The present invention relates to compounds which are intermediates in the synthesis of bile acid derivatives with pharmacological activity. The invention relates to compounds of general formula (I):wherein:, R1, R2, R3, R4, R5, R6 and Y are as defined herein.The compounds are intermediates in the synthesis of synthetic bile acids which are useful in the treatment of conditions such as liver disease. In addition, the invention relates to a method of synthesizing these intermediates and a method of preparing obeticholic acid and obeticholic acid analogues from the compounds of the invention.
专利号:WO-2024012791-A1 优先权日:2022-07-11 标题 :Electrochemical synthesis of pyrazolines and pyrazoles 发明人:BÄR ROBIN MAXIMILIAN; FORD MARK JAMES; KALDAS SHERIF JAMES; WALDVOGEL SIEGFRIED; HOFMANN SILJA; LINDEN MARTIN 权利人:BAYER AG 摘要:The present invention relates to an electrochemical process for the synthesis of pyrazolines and pyrazoles of formula (I). The process can be especially used for the synthesis of the herbicide safener mefenpyr-diethyl.
专利号:WO-2024201393-A1 优先权日:2023-03-29 标 题:Methods for the synthesis of nucleoside analogues and nucleosides analogues derived therefrom 发明人:BRITTON ROBERT; Muir Garrett; ANKETELL MATTHEW JAMES; HUXLEY COHAN; BAIKABI SUPING 权利人:UNIV FRASER SIMON 摘要:The present invention relates to methods for the synthesis of nucleoside analogues. More specifically, the present invention relates to methods for the synthesis of C4' substituted nucleoside analogues via the reaction of a soft nucleophile with a halohydrin ketone.
专利号:US-12351573-B2 优先权日:2019-05-09 标 题:Compounds for use in synthesis of peptidomimetics 发明人:AL-ABED YOUSEF; CHENG KAI FAN 权利人:FEINSTEIN INSTITUTES FOR MEDICAL RESEARCH 摘要:Synthesis of O-benzotriazole and O-imidazole synthons are described. Uses of synthons in synthesis of azapeptides and other peptidomimetics, azapeptides and other peptidomimetics synthesized from the synthons and uses of azapeptides and other peptidomimetics are also described.
专利号:WO-2013057110-A1 优先权日:2011-10-19 标 题:Method for the synthesis of citric acid esters 发明人:ALTENBACH HANS-JOSEF; LANGE KARSTEN; NANDI SUKHENDU; IHIZANE RACHID; JAKOB BERND; SCHNEIDER MANFRED 权利人:BERGISCHE UNI WUPPERTAL; ALTENBACH HANS-JOSEF; LANGE KARSTEN; NANDI SUKHENDU; IHIZANE RACHID; JAKOB BERND; SCHNEIDER MANFRED 摘要:The present invention discloses a targeted synthesis method for the synthesis of asymmetric monoesters and/or symmetrical diesters of citric acid through acidic esterification by using boric acid or a boronic acid as a catalyst. The boric/boronic acid simultaneously acts as a catalyst, as well as a 'protecting group' for the tertiary carboxylic acid, and therefore specifically only the asymmetric monoesters or symmetrical diesters are created.
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