专利号:US-8350031-B2 优先权日:2008-06-02 标 题:Processes for the synthesis of levocetirizine and intermediates for use therein 发明人:RAO DHARMARAJ RAMACHANDRA; KANKAN RAJENDRA NARAYANRAO; GHAGARE MARUTI; CHIKHALIKAR SANDIP VASANT 权利人:CIPLA LTD; RAO DHARMARAJ RAMACHANDRA; KANKAN RAJENDRA NARAYANRAO; GHAGARE MARUTI; CHIKHALIKAR SANDIP VASANT 摘要:The present invention provides a compound of formula (IV) n nwherein R is Cl, Br, NO 2 , OH or OR′, and R′ is alkyl, and its use in the synthesis of levocetirizine, including its use in the synthesis of (−)-1-[(4-chlorophenyl)-phenylmethyl]piperazine, an intermediate useful in the synthesis of levocetirizine. The present invention also provides compounds (II) and (III) which are useful in the synthesis of compound (IV).
专利号:US-5736626-A 优先权日:1996-01-29 标题:Solid support reagents for the direct synthesis of 3'-labeled polynucleotides 发明人:MULLAH KHAIRUZZAMAN BASHAR; ANDRUS WILLIAM A 权利人:PERKIN ELMER CORP 摘要:The compounds of the invention are exemplified by the class of diglycolate synthesis supports particularly useful as support reagents for the direct synthesis of 3'-labeled polynucleotides. Generally, the compounds of the invention have the structure ##STR1## where T is an acid-cleavable hydroxyl protecting group, e.g., 4,4'-dimethoxytrityl; L 1 is a linker for connecting a 3'-terminal nitrogen to carbon; L 2 and L 3 are linkers for connecting oxygen and carbon; W is a solid support, e.g., CPG or polystyrene; L 4 is a linker for connecting the solid support to nitrogen; R 1 and R 2 are nitrogen substituents, e.g., hydrogen, lower alkyl, nitrogen protecting group, or label; and R 3 through R 7 are carbon substituents, e.g., hydrogen or lower alkyl. In a first particularly preferred embodiment, the synthesis supports of the invention are exemplified by compounds having the structure ##STR2## where DMT is 4,4'-dimethoxytrityl and W is polystyrene. In a second particularly preferred embodiment, the synthesis supports of the invention are exemplified by compounds having the structure ##STR3## where DMT and W are defined above.
专利号:US-11938187-B2 优先权日:2021-06-10 标题:Methods and compositions for synthesis of two-photon cleavable phosphoramidite molecules for oligonucleotide conjugation 发明人:LO PEGGY PIK KWAN; LIU LING SUM; TAM DICK YAN 权利人:UNIV CITY HONG KONG 摘要:The syntheses of two phosphoramidite building blocks based on BNSF and BNSMB structures are disclosed. Furthermore, some common molecular intermediates have been designed and linked to the central biphenyl core of the two molecules, resulting in a versatile and cost-effective design. These compounds can be effectively introduced to DNA oligonucleotides via the well-established standard cyanoethylphosphoramidite chemistry on the nucleic acid synthesizer. Fragmentation of these BNSF- and BNSMB-functionalized DNA strands is achieved by both one-photon and two-photon photolysis of photoliable bonds of [2-(2-nitrophenyl)propoxy]carbonyl groups on BNSF and BNSMB molecules respectively, resulting in two short pieces of single-stranded DNAs. The versatile design and facile synthesis of these two-photon photocleavage phosphoramidite molecules are beneficial to synthetic chemists and photochemists for the development of new caged compounds which enables to introduce into oligonucleotides as light-triggered carriers via solid-phase synthesis for a wide range of applications in materials science, polymer, chemistry, biology and DNA nanoecthnology.
专利号:US-2004152905-A1 优先权日:2003-01-31 标题:Universal building blocks and support media for synthesis of oligonucleotides and their analogs 发明人:GUZAEV ANDREI P; MANOHARAN MUTHIAH 摘要:Compounds for the synthesis of oligomeric compounds, particularly oligonucleotides and chemically modified oligonucleotide analogs, are provided. In addition, methods for functionalization of a support medium with a first monomeric subunit and methods for the synthesis of oligomeric compounds utilizing the novel compounds bound to support media are provided.
专利号:US-2004242897-A1 优先权日:2002-07-31 标题 :Universal support media for synthesis of oligomeric compounds 发明人:GUZAEV ANDREI P; MANOHARAN MUTHIAH 摘要:Compounds for the synthesis of oligomeric compounds, particularly oligonucleotides and oligonucleotide mimetics, are provided. In addition, methods for functionalizing a support medium with a first monomeric subunit and methods for the synthesis of oligomeric compounds utilizing the novel compounds bound to support media are provided.
专利号:US-8669356-B2 优先权日:2009-10-21 标 题 :Linker and support for solid phase synthesis of nucleic acid 发明人:HAYAKAWA YOSHIHIRO; TSUKAMOTO MASAKI; MORI KENJIRO; MINOMI KENJIRO; MAETA ERI; KONISHI TATSUYA 权利人:HAYAKAWA YOSHIHIRO; TSUKAMOTO MASAKI; MORI KENJIRO; MINOMI KENJIRO; MAETA ERI; KONISHI TATSUYA; NITTO DENKO CORP; UNIV NAGOYA NAT UNIV CORP 摘要:The invention provides a universal linker capable of synthesizing nucleic acid having a phosphate group at the 3′ terminal, a universal support carrying the linker, and a synthesis method of nucleic acid using the universal support. The linker for solid phase synthesis of nucleic acid contains a compound represented by at least one of the following formulae n nwherein each symbol is as defined in the specification.
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合成参考文献
参考文献:10.1007/978-1-61779-188-8_3 摘要:Hari Y, Kodama T, Imanishi T, Obika S. 2'-O,4'-C-methyleneoxymethylene bridged nucleic acids (2',4'-BNA(COC)). Methods Mol Biol. 2011;764():31–57. doi: 10.1007/978-1-61779-188-8_3. 参考文献:10.1007/978-1-61779-188-8_18 摘要:Putta MR, Yu D, Kandimalla ER. Synthesis, purification, and characterization of immune-modulatory oligodeoxynucleotides that act as agonists of Toll-like receptor 9. Methods Mol Biol. 2011;764():263–77. doi: 10.1007/978-1-61779-188-8_18.