N,N-二(三甲基硅基)乙酰胺置于三乙胺盐酸盐体系中,100.0 °C,2.0 Kpa 条件下,反应生成N-三甲基硅基乙酰胺 参考文献:Pudovik,M.A. Et Al.,Journal Of General Chemistry Of The Ussr,1978,Vol. 48,P. 2402-2405 标题:Pudovik,M.A. Et Al.,Journal Of General Chemistry Of The Ussr,1978,Vol. 48,P. 2402-2405
专利号:WO-9407900-A1 优先权日:1992-09-25 标 题 :Synthesis of n-glycosylated compounds with the use of a mild, iodine-catalyzed reaction 发明人:KOREEDA MASATO; HOUSTON TODD A 权利人:UNIV MICHIGAN 摘要:The invention concerns N-glycosylated derivatives of nitrogen nucleophile compounds. The invention also concerns a mild, cost effective, stereoselective, regioselective, and generally applicable method for the preparation of N-glycosides by N-glycosylation of azide and amide nucleophile compounds. The method employs iodine in a catalytic amount that uniquely does not pose an environmental hazard. The invention provides efficient access to key intermediates for the synthesis inter alia of analogs of AZT and DDI and for the synthesis of conventional N-nucleoside antibiotic drugs and their novel N-glycosylated analogs.
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:EP-2607373-A1 优先权日:2011-12-23 标 题 :Liquid phase synthesis of self-assembling peptides to be linked to polymers or to other bioactive and/or self-assembling peptides 发明人:MOUSSA WAFA; JEANNIN LAURENT; CALLENS ROLAND; BOUSMANNE MARTIN 权利人:SOLVAY 摘要:The present invention relates to a process for preparing a peptide moiety comprising an amino acid sequence (I) n€ƒ€ƒ€ƒ€ƒ€ƒ€ƒ€ƒ€ƒ R-Xaa1-Xaa5-Xaa3-Xaa6-R1€ƒ€ƒ€ƒ€ƒ€ƒ(I), nwherein R1 is selected from OH and NH 2 nand a peptide moiety comprising an amino acid sequence (II) n€ƒ€ƒ€ƒ€ƒ€ƒ€ƒ€ƒ€ƒ H-Xaa1-Xaa2-Xaa3-Xaa4-Xaal-Xaa5-Xaa3-Xaa6-R1€ƒ€ƒ€ƒ€ƒ€ƒ(II), nwherein R1 is selected from OH and NH 2 nwhereby Xaa1 and Xaa3 are residues of hydrophobic amino acids and are preferably selected from the group consisting of phenylalanine, tryptophan, histidine, tyrosine, isoleucine, alanine, leucine, norleucine and valine ; and Xaa2, Xaa4, Xaa5 and Xaa6 are residues of charged amino acids and are preferably selected from the group consisting of arginine, aspartic acid, glutamic acid and lysine. The invention further relates to a process for synthesis of a polymer covalently linked with at least one peptide, wherein the peptide comprises said peptide moiety.
专利号:US-9458188-B2 优先权日:2010-12-22 标 题 :Efficient peptide couplings and their use in the synthesis and isolation of a cyclopenta (G) quinazoline trisodium salt 发明人:KERSCHEN JAMES ALAN; BRIDGES ALEXANDER JAMES; CHOUBAL MILIND D; DALZIEL SEAN MARK; JACKS THOMAS ELLIOTT; THOMPSON ANDREW S; ZELLER JAMES ROBERT 权利人:KERSCHEN JAMES ALAN; BRIDGES ALEXANDER JAMES; CHOUBAL MILIND D; DALZIEL SEAN MARK; JACKS THOMAS ELLIOTT; THOMPSON ANDREW S; ZELLER JAMES ROBERT; BTG INT LTD 摘要:A new method for the synthesis of L-Glutamyl-γ-D-Glutamic acid and its use in the synthesis of (2R)-((4S)-carboxy-4-(4,N-(((6S)-2-(hydroxymethyl)-4-oxo-3,4,7,8-tetrahydro-3H-cyclopenta[g]quinazolin-6-yl)-N-(prop-2-ynyl)amino)benzamido)butanamido)pentanedioic acid, 1 are provided. Also provided is an efficient method for the isolation and purification of the trisodium salt of the abovementioned acid, 2, in a form suitable for long term storage and use in a parenteral dosing form.
专利号:EP-2030975-A1 优先权日:2007-08-06 标 题:CEFDINIR synthesis process 发明人:MANCA ANTONIO; FILIPPI MAURO; SALA BRUNO MAURIZIO; MONGUZZI RICCARDO AMBROGIO; FOGLIATO GIOVANNI 权利人:ACS DOBFAR SPA 摘要:Cefdinir preparation by synthesis of new key intermediates, isolable as variously solvated species complexed with thiophosphoric acid derivatives or with phosphoric acid derivatives.
专利号:US-4369312-A 优先权日:1980-07-04 标 题:Method of producing oxo-containing azetidinone compounds 发明人:HASHIMOTO MASASHI; ARATANI MATSUHIKO; HAGIWARA DAIJIRO; SAWADA KOZO; ONAMI TETSUO 权利人:FUJISAWA PHARMACEUTICAL CO 摘要:This invention relates to a novel method of producing oxo-containing azetidinone compounds, or salts thereof, or hydrates thereof, said compounds having utility as antimicrobial agents and as intermediates for the synthesis of other azetidinone compounds having antimicrobial activity.
摘要:Nokami, T., Science of Synthesis Knowledge Updates, (2016) 2, 267. 摘要:Personal Communication from G.D. Stoner, Dept. of Community Medicine, School of Medicine, Univ. of California, La Jolla, CA 92037, May 25, 1975, 27MAY1975