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-11059835-B2 优先权日:2014-08-15 标 题 :Synthesis of cephalosporin compounds 发明人:WALLER DAVID; GAZDA GREGORY; MINDEN ZACHARY; BARTON LISA; LEIGH CLIFTON 权利人:MERCK SHARP & DOHME 摘要:Provided herein is a method for the synthesis of cephalosporin antibiotic compounds comprising a palladium-catalyzed coupling reaction.
专利号:US-12049470-B2 优先权日:2021-02-01 标 题 :MK2 inhibitors, the synthesis thereof, and intermediates thereto 发明人:RUCHELMAN ALEXANDER L; COOMBS JOHN R; ZHU KEMING; LIM DANIEL; JOE CANDICE LEE; GEORGE DAVID T; ZHENG BIN; LIN DONG 权利人:CELGENE CORP 摘要:The present disclosure provides novel synthetic intermediates useful in the synthesis of MK2 kinase inhibitors.
专利号:US-2015080598-A1 优先权日:2012-03-30 标题:Asymmetric synthesis for preparing fluoroleucine alkyl esters 发明人:HUMPHREY GUY; CHUNG CHEOL; RIVERA NELO; BELYK KEVIN 权利人:MERCK SHARP & DOHME 摘要:The instant invention describes a novel asymmetric synthesis of fluoroleucine alkyl esters which utilizes a phase transfer catalyst and a solid additive.
专利号:US-12234209-B2 优先权日:2018-06-25 标题 :N-alkylation of acridans 发明人:NATRAJAN ANAND 权利人:SIEMENS HEALTHCARE DIAGNOSTICS INC 摘要:The present invention provides compounds used in the synthesis of chemiluminescent acridinium compounds and methods of producing these compounds. Specifically, methods are provided for the N-alkylation of acridan compounds using alkylating reagents. Typically, these alkylating reagents comprise a protected sulfonate group protected with an acid-labile protecting group.
专利号:US-12172982-B2 优先权日:2020-08-12 标 题:Synthesis of quinazoline compounds 发明人:LIM NGIAP-KIE; SHEN JEFF; SIROIS LAUREN ELIZABETH; TIMMERMAN JACOB C; TRACHSEL ETIENNE; WHITE NICHOLAS ANDREW; XU JIE; ZHANG HAIMING; BACHMANN STEPHAN; BIGLER RAPHAEL; CLAGG KYLE BRADLEY PASCUAL; DIPASQUALE ANTONIO GIOVANNI; GOSSELIN FRANCIS; ORCEL UGO JONATHAN; MEIER ROLAND CHRISTOPH 权利人:GENENTECH INC; HOFFMANN LA ROCHE 摘要:Provided herein are methods of synthesizing quinazoline compounds comprising at least one atropisomeric center.
[参考文献]: Jisheng Zhang, Et Al. Redox Inactive Metal Ion Triggered N-Dealkylation By An Iron Catalyst With Dioxygen Activation: A Lesson From Lipoxygenases. Dalton Trans. 2015 Jun 7;44(21):9847-59.
合成参考文献
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