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-2015197503-A1 优先权日:2012-07-27 标题 :Process for the synthesis of substituted urea compounds 发明人:RUSSO DOMENICO; WAHNON JORGE BRUNO REIS; MATON WILLIAM; ESZENYI TIBOR 权利人:BIAL PORTELA & Cª S A 摘要:A process for preparing a substituted urea compound of Formula II or Formula I, or a pharmaceutically acceptable salt or ester thereof, Formula II, Formula I the process comprising the reaction of an intermediate of Formula II′ or Formula 1′, Formula II′, Formula I′ with a carbamoyl halide of the formula: R1R2NC(=0)Hal, in a solvent consisting essentially of pyridine, wherein Hal represents Cl, F, I or Br, and wherein ring A, and R1, R2, R5, V, W, X, Y and Z are as defined herein.
专利号:US-4874558-A 优先权日:1987-05-21 标 题:Polymer catalyzed synthesis of acid anhydrides 发明人:FIFE WILMER K; ZHANG ZHI-DONG 权利人:INDIANA UNIVERSITY FOUNDATION 摘要:Solid-phase copolymers of 4-vinylpyridine or 4-vinylpyridine 1-oxide may be employed as catalysts in the formation of acid anhydrides. A water soluble polymer of 4-vinylpyridine 1-oxide may also be employed as a catalyst in the formation of acid anhydrides.
专利号:US-5770752-A 优先权日:1995-12-18 标题 :Process for reducing the concentration of by-products in product mixtures 发明人:KAUFMANN WILHELM; WISSER THOMAS; STREB JOHANN; RINK THOMAS; ZENK ROLAND; RIEDEL MICHAEL; CABRERA IVAN 权利人:TARGOR GMBH 摘要:The present invention relates to a process for reducing the concentration of organometallic and/or inorganic by-products in product mixtures formed in the synthesis of metallocenes, which comprises treating a mixture comprising one or more metallocenes and one or more organometallic and/or inorganic by-products with a polar extractant.
专利号:US-6710185-B2 优先权日:2000-09-20 标 题 :Process for the preparation of cell proliferation inhibitors 发明人:GUPTA ASHOK K; KING STEVEN A; LEE ELAINE C; MORTON HOWARD E; PLATA DANIEL J; PU YU-MING; SHARMA PADAM N 权利人:ABBOTT LAB 摘要:The instant invention discloses a process for the synthesis of substituted indole cell proliferation inhibitors.
专利号:US-2002128496-A1 优先权日:2001-01-12 标题 :Process for the preparation of matrix metalloproteinase inhibitors 发明人:CHANG SOU-JENG; FERNANDO DILINIE P; GUPTA ASHOK; HILL DAVID R; WITTENBERGER STEVEN J 摘要:The present invention discloses a process for the synthesis of reverse hydroxamate matrix metalloproteinase (MMP) inhibitors.
摘要:Inamoto, K., Science of Synthesis: Cross Coupling and Heck-Type Reactions, (2012) 2, 414. 摘要:Parmeggiani, F.; Galman, J. L.; Montgomery, S. L.; Turner, N. J., Science of Synthesis, (2019) , 378. 参考文献:10.1007/s10529-008-9747-9 摘要:Miyazawa T, Houhashi M, Inoue Y, Murashima T, Yamada T. Resolution of secondary alcohols via Carica papaya lipase-catalyzed enantioselective acylation. Biotechnol Lett. 2008 Oct;30(10):1783–7. doi: 10.1007/s10529-008-9747-9.