欧盟法规
C&L通报上下游产品
2,4,6-trimethylbenzene-1-sulfonyl fluoride 1,3,5-trimethyl-benzene chlorosulfonic acid sulfuryl dichloride 1,2-bis(thiophen-2-yl)ethane 1,2-bis(3-methoxyphenyl)ethane 1,2-bis(4-methoxyphenyl)ethane 1,2-di-p-tolylethane 📜均三甲苯置于氯磺酸体系中,用79%的收率获得产物2,4-二磺酰氯基均三甲苯
参考文献:通过磷酸三酯方法使用s,S-二苯基脱氧核糖核苷3'-磷酸二硫酯和双功能缩合试剂合成寡脱氧核糖核苷酸
标题:通过磷酸三酯方法使用s,S-二苯基脱氧核糖核苷3'-磷酸二硫酯和双功能缩合试剂合成寡脱氧核糖核苷酸
摘要:合成了四种芳香二磺酰氯作为寡聚脱氧核糖核苷酸合成的缩合剂,并在胸苷基(3'-5')胸腺嘧啶核苷的合成中考察了它们的缩合能力.其中,均三甲苯二磺酰氯(mds)和异二烯丙基异磺酰氯(dds)被证明对于缩合和从同时形成的5'-磺化副产物中分离产物是有效的.本文详细描述了通过次膦酸酯从s,S-二苯基脱氧核糖核苷3'-磷酸二硫酯衍生物中选择性除去两个苯硫基之一的研究,这些衍生物已成功地用作液相合成十二烷氧基核糖核苷酸的起始结构单元,Dcattattaatac.
DOI:10.1016/s0040-4020(01)96778-X
专利信息
专利号:US-5705629-A
优先权日:1995-10-20
标 题:Methods for H-phosphonate synthesis of mono- and oligonucleotides
发明人:BHONGLE NANDKUMAR
权利人:HYBRIDON INC
摘要:New methods of synthesizing mono- and oligo- nucleotide H-phosphonates are disclosed. The methods comprise contacting a mononucleoside with phosphonic acid and benzoyl anyhydride to yield the corresponding mononucleoside H-phosphonate. Preferrably a catalytic amount of triphosgene is also used. A similar procedure can be used to couple a first mononucleoside to a second mononucleoside or to an oligonucleotide, the method comprising contacting, in the presence of benzoic anhydride and, preferrably, a catalytic amount of triphosgene, a mononucleotide or oligonucleotide having a free 5' hydroxyl with a mononucleoside having a 3' hydroxyl-bearing phosphorous moiety (preferably H-phosphonate).
专利号:WO-9817675-A1
优先权日:1996-10-18
标 题:Improved methods for h-phosphonate synthesis of mono- and oligonucleotides
发明人:BHONGLE NANDKUMAR
权利人:HYBRIDON INC
摘要:New methods of synthesizing mono- and oligo- nucleotide H-phosphonates are disclosed. The methods comprise contacting a mononucleoside with phosphonic acid and benzoyl anhydride to yield the corresponding mononucleoside H-phosphonate. Preferably, a catalytic amount of triphosgene is also used. A similar procedure can be used to couple a first mononucleoside to a second mononucleoside or to an oligonucleotide, the method comprising contacting, in the presence of benzoic anhydride and, preferably, a catalytic amount of triphosgene, a mononucleotide or oligonucleotide having a free 5'hydroxyl with a mononucleoside having a 3'hydroxyl-bearing phosphorous moiety (preferably H-phosphonate).
专利号:US-2009111737-A1
优先权日:1999-05-24
标题:Novel antibacterial agents
发明人:CHRISTENSEN BURTON G; MORAN EDMUND J; GRIFFIN JOHN H; JUDICE J KEVIN; MU YONGQI; PACE JOHN L; MAMMEN MATHAI; AGGEN JAMES
权利人:CHRISTENSEN BURTON G; MORAN EDMUND J; GRIFFIN JOHN H; JUDICE J KEVIN; MU YONGQI; PACE JOHN L; MAMMEN MATHAI; AGGEN JAMES
摘要:This invention relates to novel multibinding compounds (agents) that are antibacterial agents. The multibinding compounds of the invention comprise from 2-10 ligands covalently connected by a linker or linkers, wherein each of said ligands in their monovalent (i.e., unlinked) state have the ability to bind to a an enzyme involved in cell wall biosynthesis and metabolism, a precursor used in the synthesis of the bacterial cell wall and/or the bacterial cell surface thereby interfere with the synthesis and/or metabolism of the cell wall. In particular the multibinding compounds of the invention comprise from 2-10 ligands covalently connected by a linker or linkers, wherein each of said ligands hasn a ligand domain capable of binding to penicillin binding proteins, a transpeptidase enzyme, a substrate of a transpeptidase enzyme, a beta-lactamase enzyme, pencillinase enzyme, cephalosporinase enzyme, a transglycoslase enzyme, or a transglycosylase enzyme substrate; Preferably, the ligands are selected from the beta lactam or glycopeptide class of antibacterial agents.
专利号:WO-0102371-A1
优先权日:1999-03-05
标题:Optically active piperazine compounds, intermediates for the preparation of the same and processes for the preparation of both
发明人:INOUE TSUTOMU; SATO DAISUKE
权利人:NIPPON SODA CO; INOUE TSUTOMU; SATO DAISUKE
摘要:Optically active hydroxymethylpiperazines represented by general formula (1), useful as catalysts for asymmetric synthesis and so on; and intermediates for the preparation of the same, wherein R1 is hydrogen, alkyl, cycloalkyl, optionally substituted aralkyl or the like; R2 is hydrogen or a protecting silyl group; X is carbonyl or sulfonyl; and Y is optionally substituted alkyl, alkenyl, cycloalkyl, aryl or the like.
专利号:WO-9623808-A1
优先权日:1995-02-01
标 题 :Improved methods for h-phosphonate synthesis of oligonucleotides
专利号:CA-2205218-C
优先权日:1995-10-20
标 题 :Improved methods for h-phosphonate synthesis of mono- and oligonucleotides