专利号:US-7329515-B2 优先权日:2003-04-21 标题 :Solid support for the synthesis of 3′-amino oligonucleotides 发明人:LEUCK MICHAEL; WOLTER ANDREAS 权利人:SIGMA ALDRICH CO 摘要:The present invention discloses novel methods and solid supports for the synthesis of 3′-amino oligonucleotides. The novel supports are based on an unsubstituted or ring-substituted hydroxymethylbenzoyl linker element wherein the hydroxymethyl group is esterified to a solid phase bound carboxylic acid and the carbonyl group is linked to an amino alcohol as an amide. Oligonucleotides are conveniently synthesized on the novel supports with no modifications in the standard phosphoramidite synthesis scheme. The ester function of the support is cleaved under the alkaline deprotection conditions for oligonucleotides to provide a free hydroxymethyl group that aids in the release of the 3′-amino oligonucleotide products with a free amino group through neighbor group participation. The free amino group of the oligonucleotides is available for further conjugation reactions to haptens, reporter groups, surfaces or other small molecules or biomolecules. The methods provided are particularly mild, do not require any modifications in standard protocols for the synthesis and deprotection of oligonucleotides, provide the 3′-amino oligonucleotides free of side products and do not introduce chiral centers to the oligonucleotides.
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-2022401910-A1 优先权日:2019-12-02 标 题 :Apparatus for the synthesis of oligonucleotides and process for the preparation thereof 发明人:AEMISSEGGER ANDREAS; DUGOVIC BRANISLAV; JAUKER MARIO; STAUSS MARTIN 权利人:BACHEM AG 摘要:The present invention provides apparatuses and methods for the synthesis of oligonucleotides and related compounds. In particular, the present invention allows to effectively prepare reagents to be fed into an apparatus for the synthesis of such oligomers.
专利号:US-7705136-B2 优先权日:2005-02-25 标 题 :Synthesis of 3′-, or 5′-, or internal methacrylamido-modified oligonucleotides 发明人:GOLOVA JULIA B; CHERNOV BORIS K 权利人:UCHICAGO ARGONNE LLC 摘要:New modifiers were synthesized for incorporation of a methacrylic function in 3′-, 5′- and internal positions of oligonucleotides during solid phase synthesis. A modifier was used for synthesis of 5′-methacrylated oligonucleotides for preparation of microarrays by a co-polymerization method.
专利号:US-2024368099-A1 优先权日:2022-01-18 标 题:Methods for the synthesis of di(hydroxymethyl)tetrahydrofuran and its application in polyesters and polyurethanes 发明人:SPIEGELBERG BRIAN; BRANDT ADRIAN; BECK HORST; KUX ALEXANDER; TIN SERGEY; DE VRIES JOHANNES GERARDUS 权利人:HENKEL AG & CO KGAA 摘要:The present invention relates to the synthesis of di(hydroxymethyl)tetrahydrofuran (DHMTHF) and the preparation of trans-enriched mixtures of DHMTHF. The invention further refers to polyester polyols which are obtained by reaction of cis/trans DHMTHF mixtures with a dicarboxylic acid. The invention further relates to polyurethanes and compositions containing a polyester polyol comprising DHMTHF, in particular to such polyurethane-containing (adhesive) compositions.
专利号:US-10040752-B2 优先权日:2015-08-24 标 题 :Synthesis of levomethadone hydrochloride or dextromethadone hydrochloride and methods for use thereof 发明人:MKRTCHYAN GNEL; YAO QINGWEI 权利人:CODY LABORATORIES INC 摘要:Highly efficient methods for synthesis of levomethadone hydrochloride or dextromethadone hydrochloride are provided starting from D-alanine, or L-alanine, respectively, with retention of configuration. Methods for treating a subject are provided comprising administering a composition comprising an effective amount of levomethadone hydrochloride having not more than 10 ppm dextromethadone.
摘要:Schmidberger, J. W.; Hepworth, L. J.; Green, A. P.; Flitsch, S. L., Science of Synthesis: Biocatalysis in Organic Synthesis, (2015) 1, 336. 摘要:Hollmann, F., Science of Synthesis Knowledge Updates, (2021) 3, 437. 摘要:Besson, M.; Pinel, C., Science of Synthesis: Catalytic Reduction in Organic Synthesis, (2017) 2, 278. 摘要:Kleemann A., Kutscher B., Reichert D., Bossart M., Pharmaceutical Substances, Thieme [Online], Stuttgart, (2026). 参考文献:10.1021/jo049885d 摘要:Seidel G, Laurich D, Fürstner A. Iron-catalyzed cross-coupling reactions. A scalable synthesis of the immunosuppressive agent FTY720. J Org Chem. 2004 May 28;69(11):3950–2. doi: 10.1021/jo049885d.