专利号:US-5948789-A 优先权日:1994-07-15 标题:Process for synthesis of substituted sulphoxides 发明人:LARSSON MAGNUS ERIK; STENHEDE URBAN JAN; SOERENSEN HENRIK; VON UNGE SVERKER PER OSKAR; COTTON HANNA KRISTINA 权利人:ASTRA AB 摘要:PCT No. PCT/SE95/00818 Sec. 371 Date Jul. 14, 1995 Sec. 102(e) Date Jul. 14, 1995 PCT Filed Jul. 3, 1995 PCT Pub. No. WO96/02535 PCT Pub. Date Feb. 1, 1996A novel process for enantioselective synthesis of single enantiomers of omeprazole or its alkaline salts, of other optically pure substituted 2-(2-pyridinylmethyl-sulphinyl) -1H-benzimidazoles as well as of other structurally related sulphoxides or their alkaline salts. The claimed process is an asymmetric oxidation of a pro-chiral sulphide to the single enantiomers or an enantiomerically enriched form of the corresponding sulphoxide. The application also claims the enantiomeric sulphoxide products produced by the process and their use in medicine.
专利号:US-2011130578-A1 优先权日:2009-06-03 标题 :Stereoselective synthesis of certain trifluoromethyl-substituted alcohols 发明人:FANDRICK DANIEL R; KUZMICH DANIEL; REEVES JONATHAN T; SONG JINHUA J; TAN ZHULIN; LEE THOMAS 权利人:BOEHRINGER INGELHEIM INT 摘要:A process for stereoselective synthesis of a compound of Formula (X) or Formula (X′) n n n n n n n n n n wherein:n R 1 is an aryl group substituted with one to three substituent groups,n wherein each substituent group of R 1 is independently C 1 -C 5 alkyl, C 2 -C 5 alkenyl, C 2 -C 5 alkynyl, C 1 -C 5 alkoxy, C 1 -C 5 alkoxycarbonyl, aminocarbonyl, alkylaminocarbonyl, dialkylaminocarbonyl, C 1 -C 5 alkoxycarbonylamino, aminosulfonyl, C 1 -C 5 alkylaminosulfonyl, C 1 -C 5 dialkylaminosulfonyl, halogen, hydroxy, carboxy, cyano, trifluoromethyl, trifluoromethoxy, nitro, or C 1 -C 5 alkylthio wherein the sulfur atom is oxidized to sulfoxide or sulfone, and n R 2 and R 3 are each independently hydrogen or C 1 -C 5 alkyl.
专利号:US-6245937-B1 优先权日:1996-11-29 标题 :Liquid phase parallel synthesis of chemical libraries 发明人:CHENG SOAN; SAUNDERS JOHN 权利人:DUPONT PHARMACEUTICALS RES LAB 摘要:This invention features methods of biphasic synthesis for synthesizing combinatorial libraries and combinatorial libraries of chemical compounds utilizing the template, and combinatorial libraries of chemical compounds formed by the methods of this invention.
专利号:WO-2014148928-A1 优先权日:2013-03-21 标 题:Method for incorporating protecting acetal and acetal ester groups, and its application for the protection of hydroxyl function 发明人:MARKIEWICZ WOJCIECH; TOÅš-MARCINIAK AGNIESZKA; CHMIELEWSKI MARCIN 权利人:INST CHEMII BIOORG POLSKIEJ AKADEMII NAUK 摘要:The present invention is the method for incorporation of acetal and acetal ester groups for protection of hydroxyl function. The method is applied in particular in the processes of RNA synthesis. The method can be employed in the synthesis of nucleosides with acetal and acetal ester groups for the protection of hydroxyl functions. The method according to the invention consists of the reaction of an organic compound containing at least one hydroxyl group, soluble in an aprotic solvent, with a compound of the general formula 1, R 1 -S-CH 2 -O-R 2 (1) in the presence of SnCl 4 , in an aprotic solvent. In the second aspect, the present invention is the method of protecting the hydroxyl function, particularly in position 2', in nucleoside derivatives, based on the incorporation of an acetal or acetal ester group.
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-8183294-B2 优先权日:2005-03-14 标 题 :Process for enantioselective synthesis of single enantiomers of thio-substituted arylmethanesulfinyl derivatives by asymmetric oxidation 发明人:LOUVET PHILIPPE; SCHWEIZER DOMINIQUE 权利人:LOUVET PHILIPPE; SCHWEIZER DOMINIQUE; Cephelon France 摘要:The invention relates to a method for preparing a sulphoxide compound of formula (I) either as a single enantiomer or in an enantiomerically enriched form, comprising the steps of:n a) contacting a pro-chiral sulphide of formula (II) with a metal chiral complex, a base and an oxidizing agent in an organic solvent; and optionally b) isolating the obtained sulphoxide of formula (I). nn nwherein Ar, Y, R 1 are as defined in claim 1.
[参考文献]: My Hang V Huynh, Et Al. Aerobic Oxidation Of Methyl P-Tolyl Sulfide Catalyzed By A Remarkably Labile Heteroscorpionate Ruii-Aqua Complex, Fac-[ruii(H2O)(Dpp)(Tppm)]2+. J Am Chem Soc. 2003 Jan 15;125(2):308-9.
合成参考文献
摘要:Silva, V. L. M.; Pinto, D. C. G. A.; Santos, C. M. M.; Rocha, D. H. A., Science of Synthesis Knowledge Updates, (2022) 3, 373. 摘要:Lattanzi, A., Science of Synthesis: Stereoselective Synthesis, (2011) 3, 1002. 摘要:Lattanzi, A., Science of Synthesis: Stereoselective Synthesis, (2011) 3, 984. 摘要:Lattanzi, A., Science of Synthesis: Stereoselective Synthesis, (2011) 3, 999. 摘要:Lattanzi, A., Science of Synthesis: Stereoselective Synthesis, (2011) 3, 1000.