CAS: 320-67-2; 4-Amino-1-((2R,3R,4S,5R)-3,4-Dihydroxy-5-(Hydroxymethyl)Tetrahydrofuran-2-yl)-1,3,5-Triazin-2(1H)-One

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P-Chlorobenzoyl Azacitidine置于sodium Methylate体系中,用 甲醇 作为反应溶剂,化学反应 2.0H,以74.4%的收率获得产物5-氮杂胞苷
参考文献:阿扎胞苷甲醇化物及其制备方法和药物组合物,用途
标题:阿扎胞苷甲醇化物及其制备方法和药物组合物,用途
摘要:本发明公开了阿扎胞苷甲醇化物及其制备方法和药物组合物,用途.所述的阿扎胞苷甲醇化物中阿扎胞苷与甲醇的摩尔比为1:(0.4‑1.0),优选地,摩尔比为1:(0.4‑0.8),更优选地,为摩尔比为1:(0.4‑0.6),特别优选地,为摩尔比为1:0.5.所述的阿扎胞苷甲醇化物具有高溶解性,在水中易溶,可用作阿扎胞苷冻干制剂的原料药.

专利信息

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-2015182634-A1
优先权日:2012-12-28
标 题:Molecular Design and Chemical Synthesis of Pharmaceutical-Ligands and Pharmaceutical-Pharmaceutical Analogs with Multiple Mechanisms of Action
发明人：COYNE CODY P; BEAR RYAN; JONES TONI
权利人:COYNE CODY P; BEAR RYAN; JONES TONI
摘要:Multi-phase and single-phase chemical reaction schemes have been developed for the synthesis of pharmaceutical-ligand analogs, pharmaceutical-pharmaceutical analogs, and similar molecular-molecular analogs that possess multiple mechanisms of action. The multi-phase organic chemical reaction schemes include relatively mild reaction conditions, high end product yields, and comparatively rapid completion of chemical reactions, which are all of particular utility for the synthesis of preparations including covalent pharmaceutical-receptor ligand or pharmaceutical-immunoglobulin analogs. Examples of pharmaceutical-ligand preparations that can be synthesized utilizing the multi-step chemical reaction schemes include covalent chemotherapeutic-ligand agents that possess selective targeted delivery properties and a capacity to exert additive and synergistic levels of cytotoxic anti-neoplastic potency. Pharmaceutical-pharmaceutical analogs, including chemotherapeutic-chemotherapeutic analogs that are capable of exerting multiple mechanisms of action, can be synthesized using either of the described multi-phase or single-phase organic chemistry reaction schemes. Each of these representative examples has utility against a spectrum of disease states including, for example, neoplastic conditions such as mammary adenocarcinoma/carcinoma, ovarian carcinoma, prostatic carcinoma, intestinal carcinoma, melanoma, leukemia, myeloma, and lymphoma.

专利号:WO-2004011474-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; RAVIKUMAR VASULINGA T; KUMAR RAJU K
权利人:ISIS PHARMACEUTICALS INC; GUZAEV ANDREI P; MANOHARAN MUTHIAH; RAVIKUMAR VASULINGA T; KUMAR RAJU K
摘要:Compounds for the synthesis of oligomeric compounds, particularly oligonucleotide 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-6653468-B1
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
权利人:ISIS PHARMACEUTICALS INC
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-11858953-B2
优先权日:2018-04-04
标 题:Compositions and methods for synthesis of phosphorylated molecules
发明人：CHAPUT JOHN; LIAO JEN-YU; BALA SAIKAT
权利人:UNIV CALIFORNIA
摘要:The invention provides compositions and methods for synthesis of phosphorylated organic compounds, including nucleoside triphosphates.

专利号:WO-9612008-A1
优先权日:1994-10-13
标 题 :Synthesis of methylase-resistant genes
发明人：SKOPEK THOMAS R
权利人:MERCK & CO INC; SKOPEK THOMAS R
摘要:There is disclosed a method for the synthesis of methylase-resistant genes. The method involves making specific alterations in the coding sequence of a given gene which destroys methylase recognition sequences without altering the original gene coding information. There are also disclosed new genes, designated mrkI-mrkIX, which have been synthesized to illustrate the method.