专利号:US-7888337-B2 优先权日:2007-08-31 标 题 :Synthesis of oseltamivir containing phosphonate congeners with anti-influenza activity 发明人:WONG CHI-HUEY; FANG JIM-MIN; SHIE JIUN-JIE; CHENG YIH-SHYUN EDMOND; JAN JIA-TSRONG 权利人:ACADEMIA SINICA 摘要:Novel phosphonate compounds are described. The compounds have activity as neuraminidase inhibitors against wild-type and H274Y mutant of H1N1 and H5N1 viruses. The present disclosure also provides an enantioselective synthetic route to known neuraminidase inhibitors oseltamivir and the anti-flu drug Tamiflu®, as well as novel phosphonate compounds, via D-xylose. Another efficient and flexible synthesis of Tamiflu and the highly potent neuraminidase inhibitor Tamiphosphor was also achieved in 11 steps and >20% overall yields from the readily available fermentation product (1S-cis)-3-bromo-3,5 -cyclohexadiene-1,2-diol. Most of the reaction intermediates were obtained as crystals without tedious purification procedures. The key transformations include an initial regio- and stereoselective bromoamidation of a bromoarene cis-dihydrodiol, as well as the final palladium-catalyzed carbonylation and phosphonylation.
专利号:US-9365874-B2 优先权日:2007-08-10 标 题 :Methods for synthesis of olefins and derivatives 发明人:BURK MARK J; PHARKYA PRITI; VAN DIEN STEPHEN J; BURGARD ANTHONY P; SCHILLING CHRISTOPHE H 权利人:GENOMATICA INC 摘要:The invention provides a method of producing acrylic acid. The method includes contacting fumaric acid with a sufficient amount of ethylene in the presence of a cross-metathesis transformation catalyst to produce about two moles of acrylic acid per mole of fumaric acid. Also provided is an acrylate ester. The method includes contacting fumarate diester with a sufficient amount of ethylene in the presence of a cross-metathesis transformation catalyst to produce about two moles of acrylate ester per mole of fumarate diester. An integrated process for process for producing acrylic acid or acrylate ester is provided which couples bioproduction of fumaric acid with metathesis transformation. An acrylic acid and an acrylate ester production also is provided.
专利号:US-4000358-A 优先权日:1968-12-19 标题:Unsaturated ester-amides of halogenated alkenes 发明人:D ALELIO GAETANO F 权利人:ALELIO GAETANO F D 摘要:This invention deals with new unsaturated esteramides of alpha , beta -unsaturated polycarboxylic acids derived from halogenated alcohols of the formula wherein R is a divalent hydrocarbon moiety having at least one and no more than 10 carbon atoms, X is a member selected from the class of bromine and chlorine, and R' is a member selected from the class of hydrogen, X and a monovalent hydrocarbon containing at least one and no more than 20 carbon atoms. Typical esteramides are the maleates, fumarates, itaconates and citraconates. These monomers possess fire-retardant properties and are useful for the synthesis of polymers and copolymers.
专利号:US-8304553-B2 优先权日:2007-12-19 标题:Method of forming oseltamivir and derivatives thereof 发明人:LIU XUEWEI; MA JIMEI 权利人:LIU XUEWEI; MA JIMEI; UNIV NANYANG TECH 摘要:A process is provided for the synthesis of 4,5-diamino cyclohexene carboxylate ester (1): or a pharmaceutically acceptable salt thereof. R 1 -R 3 are a silyl-, an aliphatic, alicyclic, aromatic, arylaliphatic, or an arylalicyclic group. R 4 , R 11 and R 12 are H, a silyl-group, an aliphatic, alicyclic, aromatic, arylaliphatic, or an arylalicyclic group. 3,4-Dihydropyran compound (9): with R 5 and R 6 being suitable protecting groups, is reacted to form aldehyde (4): which is oxidized and converted to N-substituted carbamate (3): with R 7 being a suitable protecting group. (3) is, via oxazolinidone (13): converted to azido carboxylate ester (2): and then to 4,5-diamino cyclohexene carboxylate ester (1).
专利号:US-2019055337-A1 优先权日:2016-02-02 标题 :Low-cost synthesis of macromonomers 发明人:MAYS JIMMY W; KANG NAM-GOO; WANG WEIYU; WANG HUIQUN 权利人:UNIV TENNESSEE RES FOUND 摘要:Methods of preparing macromonomers, e.g., single- or double-tailed macromonomers, using radical polymerization of a first monomer in solution or in an emulsion are described. Methods of using the macromonomers in the preparation of multigraft copolymers are also described. For instance, the macromonomer prepared by radical polymerization can be used in an emulsion copolymerization with a second monomer to form a random multigraft copolymer. The random multigraft co-polymers can be superelastomers.
专利号:US-5635157-A 优先权日:1992-04-13 标 题 :Synthesis of 4-substituted-trans-1,2-diaminocyclohexyl polyaminocarboxylate metal chelating agents for the preparation of stable radiometal antibody immunoconjugates for therapy and spect and pet imaging 发明人:MEASE RONNIE C; KOLSKY KATHRYN L; MAUSNER LEONARD F; SRIVASTAVA SURESH C 摘要:Cyclohexyl chelating agents useful in forming antibody-metal conjugates useful for diagnostic and therapeutic purposes. New compounds and processes of forming these compounds are disclosed including 4-haloacetamido-trans-1,2-diaminocyclohexyl polyaminocarboxylate and 4-isothiocyanato-trans-1,2-diamino cyclohexane-N, N, N', N'-tetra acetic acid.