专利号:US-2004058888-A1 优先权日:2000-01-13 标题:Methods for synthesis of alpha-d-gal (1~>3) gal-containing oligosaccharides 发明人:BORNAGHI LAURENT; DEKANY GYULA; DRINNAN NICHOLAS BARRY; PAPAGEORGIOU JOHN; WEST MICHAEL LEO 摘要:This invention relates to reagents and methods for synthesis of biologically active di- and tri-saccharides comprising α-D-Gal(1→3)-D-Gal. In particular the invention provides novel reagents, intermediates and processes for the solution or solid phase synthesis of α-D-galactopyranosyl-(1→3)-D-galactose, and derivatives thereof. In one preferred embodiments the invention provides a protected monosaccharide building block of general formula (II): in which R 3 is methoxy or methyl; R 1 is H, benzoyl, pivaloyl, 4-chlorobenzoyl, acetyl, chloroacetyl, levulinoyl, 4-methylbenzoyl, benzyl, 3,4-methylenedioxybenzyl, 4-methoxybenzyl, 4-chlorobenzyl, 4-acetamidobenzyl, or 4-azidobenzyl; and R 2 is H, Fmoc, benzoyl, pivaloyl, 4-chlorobenzoyl, acetyl, chloroacetyl, levulinoyl, 4-methylbenzoyl, benzyl, 3,4-methylenedioxybenzyl, 4-methoxybenzyl, 4 -chlorobenzyl, 4-acetamidobenzyl, or 4-azidobenzyl.
专利号:US-2015336866-A1 优先权日:2013-01-01 标题:Synthesis of difluoromethyl ethers and sulfides 发明人:HARTWIG JOHN; FIER PATRICK 权利人:UNIV CALIFORNIA 摘要:The synthesis of difluoromethyl ethers and sulfides with a simple, non-ozone-depleting reagent is described. The difluoromethylation of phenols with this reagent occurs at room temperature within minutes with exceptional functional group tolerance. The mild conditions makes possible tandem processes for the conversion of aryl boronic acids, aryl halides and arenes to difluoromethyl ethers. Mechanistic studies support a reaction pathway involving nucleophilic attack of the phenolate to difluorocarbene.
专利号:US-6951878-B2 优先权日:1998-03-12 标 题:Benzo[b]thiophenyl or tetrahydro-benzo[b]thiophenyl modulators of protein tyrosine phosphatases (PTPases) 发明人:MOELLER NIELS PETER HUNDAHL; ANDERSEN HENRIK SUNE; IVERSEN LARS FOGH; OLSEN OLE HVILSTED; BRANNER SVEN; HOLSWORTH DANIEL DALE; BAKIR FARID; JUDGE LUKE MILBURN; AXE FRANK URBAN; JONES TODD KEVIN; RIPKA WILLIAM CHARLES; GE YU; UYEDA ROY TERUYUKI 权利人:NOVO NORDISK AS 摘要:The present invention provides novel compounds, novel compositions, methods of their use, and methods of their manufacture, where such compounds are pharmacologically useful inhibitors of Protein Tyrosine Phosphatases (PTPase's) such as PTP1B, CD45, SHP-1, SHP-2, PTPα, LAR and HePTP or the like. n The compounds are useful in the treatment of type I diabetes, type II diabetes, impaired glucose tolerance, insulin resistance, obesity, immune dysfunctions including autoimmunity diseases with dysfunctions of the coagulation system, allergic diseases including asthma, osteoporosis, proliferative disorders including cancer and psoriasis, diseases with decreased or increased synthesis or effects of growth hormone, diseases with decreased or increased synthesis of hormones or cytokines that regulate the release of/or response to growth hormone, diseases of the brain including Alzheimer's disease and schizophrenia, and infectious diseases.
专利号:US-6353112-B1 优先权日:1998-07-17 标 题:Sultams: Solid phase and other synthesis of anti-HIV compounds and compositions 发明人:BAKER DAVID C; JIANG BIN 权利人:UNIV TENNESSEE RES CORP 摘要:Biologically active sultams are disclosed which have potent anti-HIV activity. A combinational method of synthesis, which uses a solid support and variants thereof, are described. Biological compositions and method of treating mammals for viral infections with compositions comprising the sultams of the invention, especially HIV are described.
专利号:US-7569686-B1 优先权日:2006-01-27 标题:Compounds and methods for synthesis of bicyclic nucleic acid analogs 发明人:BHAT BALKRISHEN; XIA JIE; SETH PUNIT P; VASQUEZ GUILLERMO; MIGAWA MICHAEL T; ALLERSON CHARLES; PRAKASH THAZHA P; SWAYZE ERIC E 权利人:ISIS PHARMACEUTICALS INC 摘要:The present invention provides compounds and methods of using them for preparing bicyclic nucleosides. The bicyclic nucleosides are useful for preparing chemically modified oligomeric compounds. Oligomeric compounds comprising these bicyclic nucleosides have enhanced properties such as increased nuclease resistance.
专利号:US-9802952-B2 优先权日:2013-07-15 标 题:Method and apparatus for the synthesis of dihydroartemisinin and artemisinin derivatives 发明人:KOPETZKI DANIEL; MCQUADE DAVID TYLER; SEEBERGER PETER H; GILMORE KERRY 权利人:MAX-PLANCK-GESELLSCHAFT ZUR FÖRDERUNG DER WSS E V; MAX-PLANK-GESELLSCHAFT ZUR FÖRDERUNG DER WSS E V 摘要:The present invention is directed to a method for continuous production of dihydroartemisinin and also artemisinin derivatives derived from dihydroartemisinin by using artemisinin or dihydroartemisinic acid (DHAA) as starting material as well as to a continuous flow reactor for producing dihydroartemisinin as well as the artemisinin derivatives. It was found that the reduction of artemisinin to dihydroartemisinin in a continuous process requires a special kind of reactor and a special combination of reagents comprising a hydride reducing agent, at least one activator such as an inorganic activator, at least one solid base, at least one aprotic solvent and at least one C 1 -C 5 alcohol.
1: Giri SN, Siegel DM. Comparative studies of the covalent binding of [14C]-2-chloro-4-acetotoluidide by liver and kidney slices of the starling. J Appl Toxicol. 1991 Jun;11(3):223-8. Japanese.
合成参考文献
摘要:Sharma, U.; Kumar, R.; Gupta, S. S.; Chandra, D., Science of Synthesis Knowledge Updates, (2022) 2, 280. 摘要:Sharma, U.; Kumar, R.; Gupta, S. S.; Chandra, D., Science of Synthesis Knowledge Updates, (2022) 2, 281. 摘要:Inamoto, K., Science of Synthesis: Cross Coupling and Heck-Type Reactions, (2012) 2, 407. 摘要:Toxicology and Applied Pharmacology., 19(20), 1971 [] 摘要:Satoh, T.; Miura, M., Science of Synthesis: Catalytic Transformations via CH Activation, (2015) 1, 213.