专利号:US-2025188046-A1 优先权日:2023-12-08 标题:Ultrafast flow synthesis of functionalized sulfonyl fluorides and subsequent sufex connections via lithiated chemistry 发明人:KIM DONG-PYO; KANG JI-HO 权利人:POSTECH RES & BUSINESS DEV FOUND 摘要:Disclosed are ultrafast flow synthesis of functionalized sulfonyl fluorides and subsequent SuFEx connections via lithiated chemistry. In detail, a method of synthesizing an ortho-functionalized benzenesulfonyl fluoride derivative, the method comprises (a) reacting a benzenesulfonyl fluoride derivative represented by structural formula 1 with an organolithium represented by structural formula 2, thus synthesizing an intermediate represented by structural formula 3 in reaction scheme 1 and (b) reacting the intermediate with an electrophile, thus synthesizing a compound represented by structural formula 4 or a compound represented by structural formula 4′. The present disclosure enables the synthesis of several functionalized sulfonyl fluorides within a few seconds under mild temperature conditions in addition to the chemistry of Sulfonyl Fluoride Exchange (SuFEx), which is a next-generation click chemistry, so that sulfonyl fluoride, the main reactant of the SuFEx reaction, can be efficiently secured.
专利号:US-5286901-A 优先权日:1990-03-09 标题:Prescursors for and synthesis of mono- and difunctionalized acetylenes and difunctional 1,3-diynes 发明人:STANG PETER J; CRITTELL CHARLES M; WILLIAMSON BOBBY L; ZHDANKIN VIKTOR 权利人:UNIV UTAH RES FOUND 摘要:Precursors and methods for the synthesis of mono- and difunctionalized acetylenes are described. The invention includes novel tricoordinate iodonium transfer reagents and novel alkynyldi(phenyliodonium) salts, both of which are precursors for the functionalized acetylenes. The iodonium transfer reagents take the general form of mixed iodonium sulfonates PhI + (X)OSO 2 R f , where X may be OAc, NHAc, NCO, or CN. These mixed iodonium sulfonates are produced by reaction of iodosobenzene with certain substituted trimethylsilanes. n To make the alkynyldi(phenyliodonium) salt PhI + C.tbd.CI + Ph•2 R f SO 3 - ,a mixed iodonium sulfonate is reacted with a bistin acetylene of the kind R' 3 SnC.tbd.CSnR' 3 . Alternatively, the reaction may be performed with disubstituted tin diacetylenes to produce PhI + C.tbd.C-C.tbd.CI + Ph•2 R f SO 3 - to produce a dialkynyldi(phenyliodonium) salt. Subsequent reaction of a nucleophile with the alkynyldi(phenyl-iodonium) salt or dialkynyldi(phenyliodonium) salt produces a difunctional acetylene or a difunctional 1,3-diyne, respectively.
专利号:US-5506349-A 优先权日:1992-05-13 标 题 :Chemical synthesis of 2', 3'-dideoxycytidine 发明人:MATULIC-ADAMIC JASENKA 权利人:RIBOZYME PHARM INC 摘要:Method for synthesis of 2',3'-dideoxycytidine by providing 5'-silylated-2',3'-dideoxyuridine as an intermediate.
专利号:US-6603015-B2 优先权日:1999-03-29 标题:Synthesis of epothilones 发明人:GEORG GUNDA I; NAIR SAJIV K; REIFF EMILY; TUNOORI ASHOK RAO 权利人:UNIV KANSAS 摘要:Commercially feasible methods for synthesizing various epothilones precursors needed for the preparation of final epothilones are provided, including techniques for the synthesis of epothilone segment A and C precursors. Segment C precursors are prepared using starting nitriles, which can alternately be oxidized to ketones and converted, or reacted to form the diol with subsequent conversion to the segment. Segment A precursors are prepared by reacting a starting enone with a chiral catalyst to give an intermediate alcohol in high enantomeric excess, followed by conversion of the alcohol to the desired Segment A precursor.
专利号:WO-9323413-A1 优先权日:1992-05-13 标 题:Synthesis of nucleotide monomers 发明人:BEIGELMAN LEONID; MATULIC-ACADEMIC JASENKA 权利人:RIBOZYME PHARM INC 摘要:Methods for synthesis of 2',3'-dideoxycytidine, 2',3'-dideoxyguanosine, 2',3'-dideoxyadenosine, 2',3'-dideoxyinosine and 2',3'-dideoxyguanosine, and 3'-O-benzoyl-2'-deoxyribonucleoside.
专利号:US-8835476-B2 优先权日:2005-03-04 标 题:Synthesis of novel antimicrobials 发明人:WU FAN; WEAVER DONALD; BARDEN CHRIS; MCMASTER CHRISTOPHER; BYERS DAVID; HENNEBERRY ANNETTE; BAN FUQIANG 权利人:WU FAN; WEAVER DONALD; BARDEN CHRIS; MCMASTER CHRISTOPHER; BYERS DAVID; HENNEBERRY ANNETTE; BAN FUQIANG 摘要:The synthesis and activity of novel LpxA inhibitors is described, these inhibitors present antibacterial activity. The compounds were designed based on a receptor model developed using the crystal structure of LpxA and are arranged to have a favorable binding interaction at the active site of the enzyme. In particular, the compounds present the following formula (I) where V, W, X, Y and Z can be independently C, S, N or O and P1, P2 and P3 are ligands to bind to the three points of the proposed pharmacophore model. They can be chosen from a variety of groups.
参考文献:10.1007/s10646-011-0739-5 摘要:Antizar-Ladislao B, Sarkar SK, Anderson P, Peshkur T, Bhattacharya BD, Chatterjee M, Satpathy KK. Baseline of butyltin contamination in sediments of Sundarban mangrove wetland and adjacent coastal regions, India. Ecotoxicology. 2011 Nov;20(8):1975–83. doi: 10.1007/s10646-011-0739-5.