CAS: 5983-09-5; 1-((2R,5S)-5-(Hydroxymethyl)Tetrahydrofuran-2-yl)Pyrimidine-2,4(1H,3H)-Dione

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951-78-0 3416-05-5 105784-83-6

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尿嘧啶核苷置于咪唑,三(三甲基硅基)硅烷,Palladium 10% On Activated Carbon,四丁基氟化铵,氢气,Sodium Hydroxide,1,1'-偶氮(氰基环己烷)体系中,用 四氢呋喃,甲醇,N,N-二甲基甲酰胺,乙腈 作为反应溶剂,化学反应 17.0H,反应生成 2',3'-二脱氧尿苷
参考文献:合成 2',3'-双脱氧核苷和 2',3'-Didehydro-2',3'-双脱氧核苷衍生物的可持续方案
标题:合成 2',3'-双脱氧核苷和 2',3'-Didehydro-2',3'-双脱氧核苷衍生物的可持续方案
摘要:将核糖核苷转化为 2',3'-二脱氧核苷和 2',3'-二脱氢-2',3'-二脱氧核苷衍生物的改进方案,包括抗 Hiv 药物司他夫定 (D4T),扎西他滨 (Ddc) 和去羟肌苷 (Ddi) 成立.该过程涉及使用环保和低成本的试剂对黄原酸盐进行自由基脱氧.溴乙烷或 3-溴丙腈是制备核糖核苷 2',3'-双黄原酸酯的首选烷化剂.在随后的自由基脱氧反应中,三(三甲基甲硅烷基)硅烷和 1,1'-偶氮二(环己烷甲腈)分别被用来代替有害的 Bu 3 Snh 和 Aibn.此外,在 5'-O的脱保护步骤中,Tbaf 取代了樟脑磺酸.-甲硅烷基醚基团和一种酶(腺苷脱氨酶)用于将 2',3'-二脱氧腺苷转化为 2',3'-二脱氧肌苷 (Ddi),产率很高.
DOI:10.3390/molecules27133993

专利信息

专利号:US-9206209-B2
优先权日:2010-10-19
标 题:Nucleotide analogue, method of synthesis of nucleotide analogue, use of nucleotide analogue, antiviral pro-nucleotide, pharmaceutical composition
发明人：KRASZEWSKI ADAM; ROMANOWSKA JOANNA; SOBKOWSKI MICHAL; SZYMANSKA-MICHALAK AGNIESZKA; STAWINSKI JACEK; BORYSKI JERZY; LIPNIACKI ANDRZEJ; PIASEK ANDRZEJ
权利人:KRASZEWSKI ADAM; ROMANOWSKA JOANNA; SOBKOWSKI MICHAL; SZYMANSKA-MICHALAK AGNIESZKA; STAWINSKI JACEK; BORYSKI JERZY; LIPNIACKI ANDRZEJ; PIASEK ANDRZEJ; INST CHEMII BIOORG PAN; NARODOWY INST LEKOW
摘要:An exemplary emboidment is related to a pharmaceutical composition of the class of nucleotide analogues and antiviral pro-nucleotides useful in partial or complete inhibition of human immunodeficiency virus (HIV). An exemplary embodiment is expressed in the formula (XVI): n nwhere X stands for N 3 and B stands for thymidine-1-yl, or X stands for H and B stands for uracil-1-yl or adenin-1-yl or hypoxanthin-1-yl.A method of synthesis of the nucleotide analogue using a phosphorylating agent for synthesis of the nucleotide analogue is provided.

专利号:US-10925977-B2
优先权日:2006-10-05
标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications
发明人：YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S
权利人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S; CEIL POINT LLC; UNIV TEXAS
摘要:Novel methods of synthesis of chelator-targeting ligand conjugates, compositions comprising such conjugates, and therapeutic and diagnostic applications of such conjugates are disclosed. The compositions include chelator-targeting ligand conjugates optionally chelated to one or more metal ions. Methods of synthesizing these compositions in high purity are also presented. Also disclosed are methods of imaging, treating and diagnosing disease in a subject using these novel compositions, such as methods of imaging a tumor within a subject and methods of diagnosing myocardial ischemia.

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:US-12391691-B2
优先权日:2018-11-16
标题:Synthesis of key intermediate of KRAS G12C inhibitor compound
发明人：PARSONS ANDREW THOMAS; COCHRAN BRIAN MCNEIL; POWAZINIK IV WILLIAM; CAPORINI MARC ANTHONY
权利人:AMGEN INC
摘要:The present invention relates to an improved, efficient, scalable process to prepare intermediate compounds, such as compound 5M, having the structure n nuseful for the synthesis of compounds that target KRAS G12C mutations, such as

专利号:US-5506349-A
优先权日:1992-05-13
标 题 :Chemical synthesis of 2', 3'-dideoxycytidine
发明人：MATULIC-ADAMIC JASENKA
权利人:RIBOZYME PHARM INC
摘要:Method for synthesis of 2',3'-dideoxycytidine by providing 5'-silylated-2',3'-dideoxyuridine as an intermediate.

专利号:US-2025206736-A1
优先权日:2019-11-14
标题 :Synthesis of kras g12c inhibitor compound
发明人：CORBETT MICHAEL THOMAS; CAILLE SEBASTIEN
权利人:AMGEN INC
摘要:The present disclosure relates to an improved, efficient, scalable process to prepare intermediate compounds, such as 2-isopropyl-4-methylpyridin-3-amine, useful for the synthesis of compounds, such as Compound 9, for the treatment of KRAS G12C mutated cancers.