专利号:US-7820810-B2 优先权日:2007-03-19 标 题 :Process for the synthesis of 2′-O-substituted purine nulceosides 发明人:RAVIKUMAR VASULINGA 权利人:ISIS PHARMACEUTICALS INC 摘要:The present invention provides an improved process for the synthesis of 2′-O-substituted purine nucleosides. The process includes anhydro or thioanhydro ring opening of a selected 8,2′-cyclopurine nucleoside with a weak nucleophile in the presence of a Lewis acid ester, followed by reduction to afford the desired 2′-O-substituted purine nucleoside.
专利号:US-7030230-B2 优先权日:2002-10-25 标题:Process of purifying phosphoramidites 发明人:ROSS BRUCE; SONG QUANLAI 权利人:ISIS PHARMACEUTICALS INC 摘要:A process of purifying phosphoramidite precursors useful in inter alia synthesis of oligonucleotides comprises dissolving a crude phosphoramidite in a polar phase, adding a basic compound to the polar phase, adding a portion of water to the polar phase, contacting the polar phase with a first apolar phase to extract impurity into the apolar phase, separating the first apolar phase from the polar phase, adding a second aliquot of water to the polar phase, and contacting the polar phase with a second apolar phase, whereby the phosphoramidite partitions into the second apolar phase.
专利号:US-8026349-B2 优先权日:2004-08-20 标题 :Polynucleotide synthesis labeling chemistry 发明人:HARTSEL STEPHANIE A; KAISER ROBERT J; DELANEY MICHAEL O 权利人:DHARMACON INC 摘要:Methods and compositions for making nucleoside phosphoramidites and nucleic acids, including mono-, di-, and polynucleotides, comprising a linker covalently attached to a levulinyl moiety are provided. A levulinyl-protected linking moiety affords an orthogonal approach to modifying a polynucleotide during or after solid phase synthesis with a molecule of interest, for example, a conjugate or a dye.
专利号:US-2015139987-A1 优先权日:2013-11-20 标 题 :Treatment of homozygous familial hypercholesterolemia 发明人:MARTIN ROBERT L; MCWHERTER CHARLES A; O'MARA PATRICK J 权利人:CYMABAY THERAPEUTICS INC 摘要:Treatment of homozygous familial hypercholesterolemia by administration of (R)-2-(4-((2-ethoxy-3-(4-(trifluoromethyl)phenoxy)propyl)thio)-2-methylphenoxy)acetic acid or a salt thereof, optionally in combination with an MTP inhibitor, an apoB-100 synthesis inhibitor, or a PCSK9 inhibitor.
专利号:US-2008234475-A1 优先权日:2007-03-19 标题 :Process for the synthesis of 2'-o-substituted purines
专利号:KR-20220154788-A 优先权日:2020-03-16 标 题:Synthesis of 3'N nucleosides via oxime intermediates and related compounds
参考标题:Synthesis Of 2'-O-Methoxyethylguanosine Using A Novel Silicon-Based Protecting Group 作者:Ke Wen,Suetying Chow,Yogesh S. Sanghvi,Emmanuel A. Theodorakis |发布日期:2002.11.1 摘要:A Short And Efficient Synthesis Of 2'-O-Methoxyethylguanosine (8) Is Described. Central To This Strategy Is The Development Of A Novel Silicon-Based Protecting Group (Mdpscl(2), 2) Used To Protect The 3',5'-Hydroxyl Groups Of The Ribose. Silylation Of Guanosine With 2 Proceeded With Excellent Regioselectivity And In 79% Yield. Alkylation Of The 2'-Hydroxyl Group Of 6 Proceeded With Methoxyethyl Bromide
合成参考文献
参考文献:10.1021/jo025970e 摘要:Wen K, Chow S, Sanghvi YS, Theodorakis EA. Synthesis of 2'-O-methoxyethylguanosine using a novel silicon-based protecting group. J Org Chem. 2002 Nov 01;67(22):7887–9. doi: 10.1021/jo025970e. 参考文献:10.1080/15257770802271748 摘要:Taj SAS, Narayanan S, Meenakshi SS, Sanghvi YS, Ross BS, Ravikumar VT. Process Research on the Preparation of DMT Protected 2′-O-Methoxyethylguanosine for Oligonucleotide Synthesis in Therapeutic Applications. Nucleosides, Nucleotides and Nucleic Acids. 2008 Aug 18;27(9):1024–33. doi: 10.1080/15257770802271748.