专利号:US-9475757-B2 优先权日:2013-05-03 标 题 :Synthesis of anti-Parkinson agent 发明人:MUTHUKRISHNAN MURUGAN; MUJAHID MOHAMMAD 权利人:COUNCIL SCIENT IND RES 摘要:The present invention relates to an improved process for synthesis of anti-Parkinson compound of formula (I) from commercially available (R)-benzyl glycidyl ether, wherein the compound obtained has enantiopurity greater than >98%. Formula (I) wherein R 1 and R 2 are each independently selected from hydrogen or halogen.
专利号:US-6906046-B2 优先权日:2000-12-22 标题 :Pharmaceutical uses and synthesis of benzobicyclooctanes 发明人:JACKSON RANDY W; DARWISH IHAB; BAUGHMAN TED A; HOWBERT J JEFFRY 权利人:CELLTECH R & D INC 摘要:Benzobicyclooctane compounds, their use in inhibiting cellular events involving TNF-α and IL-8, and in the treatment of inflammation events in general; a combinatorial library of diverse bicyclooctanes and process for their synthesis as a library and as individual compounds.
专利号:US-8106031-B2 优先权日:2006-05-02 标题:Hydrolytically-resistant boron-containing therapeutics and methods of use 发明人:LEE VING; PLATTNER JACOB J; BENKOVIC STEPHEN J; BAKER STEPHEN J; MAPLES KIRK R; BELLINGER-KAWAHARA CAROLYN; AKAMA TSUTOMU; ZHANG YONG-KANG; SINGH RAJESHWAR; SAURO VITTORIO A 权利人:LEE VING; PLATTNER JACOB J; BENKOVIC STEPHEN J; BAKER STEPHEN J; MAPLES KIRK R; BELLINGER-KAWAHARA CAROLYN; AKAMA TSUTOMU; ZHANG YONG-KANG; SINGH RAJESHWAR; SAURO VITTORIO A; ANACOR PHARMACEUTICALS INC 摘要:Compositions and methods of use of boron derivatives, including benzoxaboroles, benzazaboroles and benzthiaboroles, as therapeutic agents for treatment of diseases caused by fungi, yeast, bacteria or viruses are disclosed, as well as methods for synthesis of said agents and compositions thereof.
专利号:US-7148362-B2 优先权日:2003-09-18 标题:Process for the preparation of enantiopure pyrrolidin-2-one derivatives 发明人:IDING HANS; KRUMMENACHER DANIELA; WIRZ BEAT; WOSTL WOLFGANG 权利人:HOFFMANN LA ROCHE 摘要:The present invention relates to a process for the preparation of enantiopure intermediates useful in the synthesis of valuable pharmaceutically active compounds, e.g. MAOB inhibitors, and to novel intermediates of formulae I and II n nwherein R 21 , R 22 , R 23 and R 24 are as defined in the description and claims.
专利号:US-7151112-B1 优先权日:2001-09-04 标题:Pharmaceutical uses and synthesis of nicotinamides 发明人:CUTSHALL NEIL S; JEFFREY SCOTT C 权利人:UCB SA 摘要:This invention is directed to methods of using a compound of the formula n nand pharmaceutically acceptable salts thereof, wherein n, X, R 1 and R 2 are disclosed herein, for treating inflammatory events in an animal subject.
专利号:US-2004053999-A1 优先权日:1997-09-17 标题 :Novel compounds and methods for synthesis and therapy 发明人:BISCHOFBERGER NORBERT W; DAHL TERRENCE C; HITCHCOCK MICHAEL J M; KIM CHOUNG U; LEW WILLARD; LIU HONGTAO; MILLS ROGER G; WILLIAMS MATTHEW A 摘要:Novel compounds are described. The compounds generally comprise an acidic group, a basic group, a substituted amino or N-acyl and a group having an optionally hydroxylated alkane moiety. Pharmaceutical compositions comprising the inhibitors of the invention are also described. Methods of inhibiting neuraminidase in samples suspected of containing neuraminidase are also described. Antigenic materials, polymers, antibodies, conjugates of the compounds of the invention with labels, and assay methods for detecting neuraminidase activity are also described.
[参考文献]: Patricia Ferreira, Et Al. Aryl-Alcohol Oxidase Involved In Lignin Degradation: A Mechanistic Study Based On Steady And Pre-Steady State Kinetics And Primary And Solvent Isotope Effects With Two Alcohol Substrates. J Biol Chem. 2009 Sep 11;284(37):24840-7.
合成参考文献
摘要:Hollmann, F., Science of Synthesis Knowledge Updates, (2021) 3, 437. 摘要:Singh, F. V.; Wirth, T., Science of Synthesis: Catalytic Oxidation in Organic Synthesis, (2017) 1, 45. 摘要:Parmeggiani, F.; Galman, J. L.; Montgomery, S. L.; Turner, N. J., Science of Synthesis, (2019) , 398.