专利号:US-6518438-B2 优先权日:1996-08-23 标题:Preparation of cyclohexene carboxylate derivatives 发明人:KENT KENNETH M; KIM CHOUNG U; MCGEE LAWRENCE R; MUNGER JOHN D; PRISBE ERNEST J; POSTICH MICHAEL J; ROHLOFF JOHN C; KELLY DAPHNE E; WILLIAMS MATTHEW A; ZHANG LIJUN 权利人:GILEAD SCIENCES INC 摘要:The present invention provides new synthetic methods and compositions. In particular, new methods of preparing intermediates useful in the synthesis of neuraminidase inhibitors and compositions useful as intermediates that are themselves useful in the synthesis of neuraminidase inhibitors are provided.
专利号:US-9150498-B2 优先权日:2011-10-25 标题:Process for the preparation of oseltamivir and methyl 3-epi-shikimate 发明人:RAWAT VARUN; DEY SOUMEN; ARUMUGAM SUDALAI 权利人:COUNCIL SCIENT IND RES 摘要:The present invention discloses high yielding enantioselective process for synthesis of Oseltamivir from readily available starting material, cis-1,4-butene diol. The process features incorporation of chirality using sharpless asymmetric epoxidation (AE) and diastereoselective Barbier allylation and construction of cyclohexene carboxylic acid ester core through a ring closing metathesis (RCM) reaction. Further also disclosed herein is synthesis of (−)-methyl 3-epi-shikimate.
专利号:US-7473798-B2 优先权日:2005-12-28 标题:Derivatives of unsaturated, cyclic organic acids 发明人:GABEL RICHARD A; GROANING MICHAEL D; JOHNSTON DAVID A 权利人:ROCHE PALO ALTO LLC 摘要:The present invention relates to technology for preparing derivatives of unsaturated, cyclic, organic acids and salts, thereof. Shikimic acid is an example of such an acid. More particularly, the present invention relates to preparing derivatives of these acids or salts thereof that are esterified, ketalized, functionalized with a leaving group, and/or provided with epoxide functionality. Preferred aspects may be used in the synthesis of Oseltamivir Phosphate starting from shikimic acid.
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.