专利号:WO-2008151306-A1 优先权日:2007-06-05 标题 :Synthesis of cyclodepsipeptide compounds having antineoplastic and/or antimicrobial activity 发明人:PETTIT GEORGE R; SMITH THOMAS H; FENG SONG 权利人:UNIV ARIZONA; PETTIT GEORGE R; SMITH THOMAS H; FENG SONG 摘要:The present invention is directed to effective methods of synthesizing cyclodepsipeptide compounds having antineoplastic and/or antimicrobial activity. Total syntheses of the eighteen-membered ring cyclodepsipeptides kitastatin (1a) and respirantin (1b) are taught. One important step in the synthesis is an intramolecular transesterification of the ?-ketoester alcohol 6 to afford the protected macrocycle 5. The synthetic products were shown to be identical to the natural products and the absolute stereochemistry of 6 of the 7 asymmetric centers of cyclodepsipeptide 1b was unequivocally established. Kitastatin (1a) and respirantin (1b) were found to be remarkable inhibitors of cancer cell growth and are related to the antimycin family of antibiotics.
专利号:US-6033882-A 优先权日:1994-07-07 标题:Chiral synthesis of 2-hydroxy carboxylic acids with a dehydrogenase 发明人:HOLBROOK JOSEPH JOHN; WILLIS CHRISTINE LOUISE; JOHNSEN KEYJI; HATELEY MARTIN JOHN 权利人:GENZYME CORP 摘要:PCT No. PCT/EP95/02692 Sec. 371 Date May 29, 1997 Sec. 102(e) Date May 29, 1997 PCT Filed Jul. 7, 1995 PCT Pub. No. WO96/01892 PCT Pub. Date Jan. 25, 1996Inter alia, an enzyme, a 2-hydroxy carboxylic acid dehydrogenase, characterised in that it is obtainable from Lactobacillus delbrueckii ssp. Bulgaricus and in that it catalyses the production of (R)-hydroxy derivatives of 2-keto acids, which are unsubstituted in the 3-position, but which may be substituted in the 4-position or beyond is disclosed.
专利号:US-2009123983-A1 优先权日:2007-10-03 标 题:Processes for preparing an intermediate of sitagliptin via enzymatic reduction 发明人:NIDDAM-HILDESHEIM VALERIE 权利人:NIDDAM-HILDESHEIM VALERIE 摘要:The invention provides enzymatic reduction processes for the preparation of 4-(2,4,5-trifluorophenyl)-3-hydroxybutanoate, particularly, (S)-methyl 4-(2,4,5-trifluorophenyl)-3-hydroxybutanoate, a key intermediate in the synthesis of Sitagliptin, and the (S)- and (R)-enantiomers of methyl 4-(2,4,5-trifluorophenyl)-3-hydroxybutanoate in high enantiomeric purity.
专利号:US-2004110228-A1 优先权日:2002-04-01 标 题:Combinatorial organic synthesis of unique biologically active compounds 发明人:MCALPINE SHELLI R; TAYLOR RACHEL E; BOLLA MEGAN L; SEGALL ANCA M 摘要:The invention provides a method for making a combinatorial library of cyclic compounds, such as Holliday junction-trapping compounds, comprising the steps of (a) obtaining a plurality of trimers according to the generic structure X 1- X 2- X 3 , wherein X 1 , X 2 and X 3 can be independently any naturally or nonnaturally occurring amino acids or peptidomimetics thereof; (b) optionally coupling a spacer S to the trimer at either end; (c) cyclizing two trimers or trimer-spacer conjugates in a head-to-tail orientation; thereby obtaining a combinatorial library of compounds, wherein the library does not include an unmodifed or naturally occurring Holliday Junction-trapping compounds. The invention additionally provides methods macrocyclic compounds that are synergimycin derivatives.
专利号:US-11530204-B2 优先权日:2019-09-30 标 题 :Biocatalytic synthesis of cryptophycin anticancer agents 发明人:SHERMAN DAVID H; SCHMIDT JENNIFER J 权利人:UNIV MICHIGAN REGENTS 摘要:The disclosure provides cryptophycin intermediates, cryptophycin analogs, and cryptophycin chimeric molecules useful in treating cancer, as well as methods of producing these compounds and methods of treating cancer.
专利号:WO-9522519-A1 优先权日:1994-02-17 标题 :Synthesis of polyhydroxy fatty acid amides from triglycerides 发明人:SCHEIBEL JEFFREY JOHN; REILMAN RANDALL THOMAS; SHERMAN JOE FREDERICK 权利人:PROCTER & GAMBLE 摘要:Fats and oils such as hardened palm kernel oil are reacted directly with N-substituted polyhydroxy amines to provide high yields of N-substituted polyhydroxy fatty acid amide surfactants having improved odors and low fatty acid content. Hardened palm kernel oil is reacted with N-methylglucamine in the presence of an ethoxylated alcohol, but in the absence of methanol solvent, using sodium propylene glycolate catalyst to provide the mixed corresponding fatty acid amide of N-methylglucamine.
摘要:Dornan, L. M.; Hughes, N. L.; Muldoon, M. J., Science of Synthesis: Catalytic Oxidation in Organic Synthesis, (2017) 1, 559. 摘要:Parmeggiani, F.; Galman, J. L.; Montgomery, S. L.; Turner, N. J., Science of Synthesis, (2019) , 404. 参考文献:10.1371/journal.pone.0097864|10.1371/journal.pone.0101859 摘要:Nieminen MT, Novak-Frazer L, Rautemaa V, Rajendran R, Sorsa T, Ramage G, Bowyer P, Rautemaa R. A Novel Antifungal Is Active against Candida albicans Biofilms and Inhibits Mutagenic Acetaldehyde Production In Vitro. PLoS ONE. 2014 May 27;9(5):e97864. doi: 10.1371/journal.pone.0097864.