专利号:EP-4092127-A1 优先权日:2021-05-18 标题:Enzyme-catalytic method for the direct stereoselective synthesis of gamma-(acyloxy) carboxylic acids 发明人:PARVE JAAN; KUDRJASHOVA MARINA; GATHERGOOD NICHOLAS; PARVE OMAR 权利人:TALLINN UNIV OF TECHNOLOGY 摘要:The present invention is a method for the stereoselective straightforward synthesis of gamma-acyloxy carboxylic acids of novel structure starting from racemic gamma-hydroxy carboxylic acid salts that are obtained by alkaline hydrolysis of the racemic gamma-lactones. The salt is acylated by enzyme catalysis in an organic solvent containing an acyl donor and an immobilised lipase, on stirring at room temperature (ca 20 °C) until reaching the conversion rate required. After that, the reaction mixture is acidified and extracted and the product treated with catalytic amount of para-toluenesulfonic acid in toluene during the time required for the relactonisation of the unreacted salt enantiomer. Thereafter, the target gamma-acyloxy carboxylic acid formed from one enantiomer of the starting compound and relactonised gamma-lactone formed from the other, unreacted enantiomer of the starting compound are isolated using a routine separation method, such as distillation, extraction with NaHCO3 water solution followed by acidification or column chromatography.
专利号:US-2024158926-A1 优先权日:2022-11-03 标 题 :Electrochemical synthesis of hydroxyvaleric acid from levulinic acid 发明人:HOLEWINSKI ADAM; DE SOUZA LUCAS FRANCISCO WILLIAN 权利人:UNIV COLORADO REGENTS 摘要:Disclosed herein are methods of electrochemical synthesis of hydroxyvaleric acid from levulinic acid. For example, disclosed herein are methods comprising electrochemical synthesis of hydroxyvaleric acid from levulinic acid, wherein the method is conducted in an electrochemical cell wherein a working electrode is in electrochemical contact with an aqueous electrolyte and levulinic acid, wherein the method comprises applying a potential to electrochemically reduce the levulinic acid to form hydroxyvaleric acid. Also disclosed herein are methods of synthesizing gamma-valerolactone from hydroxyvaleric acid, the method comprising acid-catalyzed esterification. Also disclosed herein are methods of use of the products produced by any of the methods herein.
专利号:US-2016200665-A1 优先权日:2013-08-21 标 题:Synthesis of biphenylalaninol via novel intermediates 发明人:ZIMMERMANN AXEL; HERMSEN PETRUS JOHANNES; HANBAUER MARTIN HELMUT FRIEDRICH 权利人:DPX HOLDINGS BV 摘要:The invention relates to a novel synthesis route towards R-biphenylalaninol and to the intermediates applied in this synthesis route. The process according to the invention and the intermediate compounds are useful in the synthesis of pharmaceutically active compounds.
专利号:US-5549974-A 优先权日:1994-06-23 标题:Methods for the solid phase synthesis of thiazolidinones, metathiazanones, and derivatives thereof 发明人:HOLMES CHRISTOPHER P 权利人:AFFYMAX TECH NV 摘要:The invention provides an efficient and versatile method for the combinatorial synthesis and screening of libraries of 4-thiazolidinones, metathiazanones, and derivatives thereof. In order to expediently synthesize a combinatorial library of derivatives based upon these core structures, a general methodology for the solid phase synthesis of these derivatives is also provided. Arrays of thiazolidinones, metathiazanones, and derivatives thereof useful as peptidomimetics and for the identification of agents having antifungal, antihistaminic, or antimicrobial activity or use in the treatment of inflammation, hypertension, renal failure, congestive heart failure, uremia and other conditions can be prepared using this method.
专利号:US-7317129-B2 优先权日:2002-06-07 标 题:Chemical synthesis of reagents for peptide coupling 发明人:RAINES RONALD T; KIESSLING LAURA L; NILSSON BRADLEY L; HE YI; SOELLNER MATTHEW B; HINKLIN RONALD J 权利人:WISCONSIN ALUMNI RES FOUND 摘要:The present invention provides improved methods for synthesis of phosphinothiol reagents, as well as novel protected reagents, for use in formation of amide bonds, and particularly, for peptide ligation. The invention provides phosphine-borane complexes useful as reagents in the formation of amide bonds, particularly for the formation of an amide bond between any two of an amino acid, a peptide, or a protein.
专利号:US-2003138880-A1 优先权日:2001-08-24 标 题:Solid-phase synthesis of oligosaccharides and glycopeptides using glycosynthases 发明人:WITHERS STEPHEN G; JENSEN KNUD J; PETERSEN LARS; TOLBORG JAKOB L 权利人:UNIV BRITISH COLUMBIA 摘要:The present invention provides materials and methods for the solid-phase synthesis of oligosaccharides and glycopeptides. Such materials and methods include mutant glycosidase enzymes, or “glycosynthases,â€? chemically-derivatized acceptor molecules, and specific solid support matrices.