专利号:US-8153361-B1 优先权日:2006-02-06 标题:Dynamic and combinatorial synthesis of polymerase primers 发明人:BENNER STEVEN ALBERT 权利人:BENNER STEVEN ALBERT 摘要:This invention relates to the field of nucleic acid chemistry, more specifically to compositions of matter that are nucleic acid analogs, and processes that use them. Still more specifically, these compositions comprise two fragments of DNA-like molecules, each having one or more ends modified to carry a reactive group, where the reactive group on one fragment can form a transient covalent bond with the reactive group on the other under conditions of dynamic equilibrium to form a composite, where the composite can then bind to a target oligonucleotide, such as a DNA or RNA molecule. Most specifically, once the transient covalent bond forms, the composite serves as a primer for a template-directed polymerization using a DNA polymerase, an RNA polymerase, or a reverse transcriptase. Once incorporated, the epimerization causes the base pair to be destabilized, the duplex containing the epimerized nucleoside to likewise be destabilized, and the double strand to then disassociate. This leaves the template available to template the synthesis of another complementary oligonucleotide containing the epimerizing base.
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-7256300-B2 优先权日:2004-03-30 标 题:Stereoselective synthesis of certain trifluoromethyl-substituted alcohols 发明人:LEE THOMAS WAI-HO; PROUDFOOT JOHN ROBERT 权利人:BOEHRINGER INGELHEIM PHARMA 摘要:A process for stereoselective synthesis of a compound of Formula (X) or Formula (X′) n nwherein R 1 , R 2 , and R 3 are as defined herein, the process comprising:n (a) reacting the starting material of formula A with a chiral sulfoxide anion source in a suitable solvent to prepare a compound of formula C or C′; (b) reducing the sulfoxide of formula C or C′ in a suitable solvent to obtain the compound of formula D or D′; and (c) cyclizing the compound of formula D or D′ in a suitable solvent to form the epoxide compound of Formula (X) or Formula (X′),n nor a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.
专利号:US-7321070-B2 优先权日:2003-07-30 标题:Synthesis of isotopically labeled R- or S-[13C, 2H] glycerols 发明人:MARTINEZ RODOLFO A; UNKEFER CLIFFORD J; ALVAREZ MARC A 权利人:LOS ALAMOS NAT SECURITY LLC 摘要:The present invention is directed to asymmetric chiral labeled glycerols including at least one chiral atom, from one to two 13 C atoms and from zero to four deuterium atoms bonded directly to a carbon atom, e.g., (2S) [1,2- 13 C 2 ]glycerol and (2R) [1,2- 13 C 2 ]glycerol, and to the use of such chiral glycerols in the preparation of labeled amino acids.
专利号:US-6417374-B1 优先权日:2001-02-15 标题 :Process for the preparation of beta hydroxy-delta lactone using novel intermediates 发明人:GHORPADE SANDEEP RAGHUNATH; KALKOTE UTTAM RAMRAO; CHAVAN SUBHASH PRATAPRAO; BHIDE SUNIL RAMCHANDRA; RAVINDRANATHAN THOTTAPPILLIL 权利人:COUNCIL SCIENT IND RES 摘要:The present invention relates to a process for the preparation of optically active 6-hydroxymethyl-4-(tert-butyldimethylsilyloxy)-(4R,6S)-tetrahydro-2H-2-pyranone(β-Hydroxy-δ-lactone) an important intermediate in the synthesis of biologically active drugs e.g. compactin, atorvastatin, fluvastatin, cholesterol lowering drugs.
专利号:US-2005234250-A1 优先权日:2004-03-30 标题 :Stereoselective synthesis of certain trifluoromethyl-substituted alcohols
参考标题:A Route To "All-Cis" 2-Methyl-6-Substituted Piperidin-3-Ol Alkaloids From Syn-(2R,1′s)-2-(1-Dibenzylaminomethyl)Epoxide: Rapid Total Synthesis Of (+)-Deoxocassine 作者:Pierre-Yves Géant,Jean Martínez,Xavier J. Salom-Roig |发布日期:2012.1 摘要:To The Synthesis Of Two Cis-2-Methyl-6-Substituted Piperidin-3-Ols Is Described. Syn-(2R,1′s)-2-(1-Dibenzylaminomethyl) Epoxide (13) Was Used As Common Building Block. The Key Step Involved Oxirane Ring Opening Of 13 By The Nucleophilic Lithium Aza-Enolate Of Hydrazones 12A And 12B. Subsequent Hydrazone Hydrolysis And Intramolecular Reductive Amination Afforded The Alkaloid (+)-Deoxocassine And A New
合成参考文献
摘要:Coote, S. C.; Smith, L. H. S.; Procter, D. J., Science of Synthesis Knowledge Updates, (2010) 3, 429. 摘要:Lattanzi, A., Science of Synthesis: Stereoselective Synthesis, (2011) 3, 984. 摘要:Lattanzi, A., Science of Synthesis: Stereoselective Synthesis, (2011) 3, 976. 摘要:Buitrago Santanilla, A.; Leighton, J. L., Science of Synthesis: Stereoselective Synthesis, (2011) 2, 432. 摘要:Grogan, G., Science of Synthesis: Biocatalysis in Organic Synthesis, (2015) 3, 286.