专利号:US-2007015260-A1 优先权日:2002-03-14 标 题:Synthesis of synthons for the manufacture of bioactive compounds 发明人:WONG CHI-HUEY; LIU JUNJIE; DESANTIS GRACE; BURK MARK 权利人:SCRIPPS RESEARCH INST 摘要:The present invention is based on the discovery that 2-deoxyribose-5-phosphate aldolase (DERA, EC 4.1.2.4) and variants thereof can be used to catalyze sequential asymmetric aldol reactions between a wide variety of donor and acceptor aldehydes. The reaction products typically contain at least two new stereogenic centers and can be produced in enantiomerically pure form. As such, DERA catalyzed asymmetric aldol chemistry can be exploited to produce synthons for the synthesis of a variety of bioactive molecules.
专利号:US-12037623-B2 优先权日:2018-07-09 标 题 :Enzymatic synthesis of 4′-ethynyl nucleoside analogs 发明人:HUFFMAN MARK A; FRYSZKOWSKA ANNA; KOLEV JOSHUA N; DEVINE PAUL N; CAMPOS KEVIN R; TRUPPO MATTHEW; NAWRAT CHRISTOPHER C 权利人:MERCK SHARP & DOHME; MERCK SHARP & DOHME LLC 摘要:The present invention relates to an enzymatic synthesis of 4′-ethynyl-2′-deoxy nucleosides and analogs thereof, for example EFdA, that eliminates the use of protecting groups on the intermediates, improves the stereoselectivity of glycosylation and reduces the number of process steps needed to make said compounds. It also relates to the novel intermediates employed in the process.
专利号:US-9181292-B2 优先权日:2011-01-05 标题 :Methods for preparation of glycosphingolipids and uses thereof 发明人:LIANG PI-HUI 权利人:LIANG PI-HUI 摘要:Methods for synthesis and preparation of alpha-glycosphingolipids are provided. Methods for synthesis of α-galactosyl ceramide, and pharmaceutically active analogs and variants thereof are provided. Novel alpha-glycosphingolipids are provided, wherein the compounds are immunogenic compounds which serve as ligands for NKT (natural killer T) cells.
专利号:US-4216171-A 优先权日:1977-11-21 标题:Novel compositions having a base of aminoalkoxy amines 发明人:LE LUDEC JOEL; SOULA GERARD 权利人:RHONE POULENC IND 摘要:Compositions containing at least one aminoalkoxy amine of the formula: (I) in which x is a whole number of from 1 to 3, are provided. They are prepared by cyanoethylation of tris(5-hydroxy-3-oxa-pentyl)amine with acrylonitrile followed by hydrogenation. They are useful as manufacturing intermediates, additives for lubricating oils, and in the synthesis of polyurethanes.
专利号:US-6664282-B2 优先权日:1999-09-17 标 题:Synthesis of [3,5,7]-1H-imidazo [1,5-a]imidazol-2 (3H)- one compounds 发明人:ELABDELLAOUI HASSAN M; OSTRESH JOHN M; HOUGHTEN RICHARD A 权利人:TORREY PINES INST 摘要:Individual substituted [3,5,7]-1H-imidazo[1,5-a]imidazol-2(3H)-one compounds and their pharmaceutically-acceptable salts are disclosed, as are libraries of such compounds. Methods of preparing and using the libraries of compounds as well as individual compounds of the libraries are also disclosed.
专利号:US-3553260-A 优先权日:1967-05-29 标 题 :Radiopaque derivatives of alpha-phenoxy-phenylacetic acid 发明人:FELDER ERNST; PITRE DAVIDE 权利人:BRACCO IND CHIMICA SPA 摘要:A - (3 - N-ALKYL-N-ACETYLAMINO-2,4,6-TRIIODOPHENOXY)PHENYLACETIC ACID AND CLOSELY RELATED DERIVATIVES OF THE FORMULA 1,3,5-TRI(I-),2-((R3-PHENYL)-CH(-COOH)-O-),4-(R2-CO- N(-R1)-)BENZENE WHEREIN R1 IS LOWER ALKYL, R2 IS HYDROGEN OR LOWER ALKYL, AND R3 IS HYDROGEN, HALOGEN OR LOWER ALKYL, AND THE PHYSIOLOGICALLY TOLERATED, WATER SOLUBLE METAL OR AMINE SALTS THEREOF ARE RADIOPAQUE, TEND TO ACCUMULATE IN THE GALL BLADDER WHEN APPLIIED ORALLY, AND ARE NON-TOXIC IN EFFECTIVE AMOUNTS. THE CORRESPONDING LOWER ALKYL ESTERS ARE INTERMEDIATES IN THE SYNTHESIS OF THE ACIDS AND SALTS.
摘要:Molander, G. A.; Ryu, D., Science of Synthesis: C-1 Building Blocks in Organic Synthesis, (2013) 2, 45. 摘要:Zhang, M.; Su, W., Science of Synthesis: Catalytic Transformations via CH Activation, (2015) 1, 96. 摘要:Schiltz, P.; Gosmini, C., Science of Synthesis: Special Topics, (2021) 1, 92. 摘要:Parmeggiani, F.; Galman, J. L.; Montgomery, S. L.; Turner, N. J., Science of Synthesis, (2019) , 402. 摘要:Schiltz, P.; Gosmini, C., Science of Synthesis: Special Topics, (2021) 1, 91.