CAS: 2341-22-2; 4-Amino-1-((2R,3R,4S,5R)-3,4-Dihydroxy-5-(Hydroxymethyl)Tetrahydrofuran-2-yl)-5-Fluoropyrimidin-2(1H)-One

该化合物是细胞胺的核核素类比,其特点是在青糖环的5处放置处替换氟原子,改变其生物特性,使其对癌症研究和抗病毒疗法感兴趣.5-氟二甲胺的分子配方为C9H11FN2O5,其分子重量反映其结构.作为核素,该产品包括一个与糖相连的基(5-含氟丙烯基).5-全氟基丁已知会干扰RNA合成,并可通过破坏正常的核酸新陈代谢抑制某些癌症细胞的生长.经常研究该分子配型在混合疗法中的潜在用途,特别是在固体肿瘤和病毒感染的治疗中.该化合物通常在制药环境中管理,其功效和安全特征是正在进行的研究的主题.与许多核糖类相比,其行动机制涉及将核素结合到RNA,导致断裂蛋白综合和最终细胞死亡.

结构式图片

相似化合物

66335-38-4 66335-38-4 65-46-3

欧盟法规

ECHA物质C&L通报

上下游产品

CAS号2560-60-3 1-(2,3,5-tri-O-... | CAS号669055-50-9 1-(β-D-xylofura... | CAS号14215-97-5 1-O-乙酰基-2,3,5-三... | CAS号316-46-1 5-氟尿嘧啶核苷 | CAS号55474-11-8 Uridine, 5-fluo... | CAS号4105-38-8 2,3,5-三乙酰尿苷 | CAS号37717-21-8 氟西他宾

合成工艺路线路线简述

    2',3',5'-三乙酰尿苷置于ammonium Hydroxide,氮,氨,Fluorine体系中,用 1,4-二氧六环,甲醇,溶剂黄146 用作溶剂,化学反应 1.5H,反应生成5-氟胞嘧啶核苷
    参考文献:Krug,A.; Schmidt,S.; Lekschas,J.,Journal Fur Praktische Chemie (Leipzig 1954),1989,Vol. 331,# 5,P. 835-842
    标题:Krug,A.; Schmidt,S.; Lekschas,J.,Journal Fur Praktische Chemie (Leipzig 1954),1989,Vol. 331,# 5,P. 835-842

    海关参考信息

    专利信息


    专利号:US-7230101-B1
    优先权日:2002-08-28
    标 题:Synthesis of methotrexate-containing heterodimeric molecules
    发明人:MURTHI KRISHNA K; SMITH CHASE C
    权利人:GPC BIOTECH INC
    摘要:The present invention relates to novel compositions of methotrexate-containing heterodimeric probe molecules, also known as chemical inducers of dimerization (CID), useful in three-hybrid assays. The invention further relates to synthesis of said compositions and their intermediates. Another aspect of the invention is a method for using the heterodimeric probe molecules described herein in drug screens to identify potential protein targets to a given ligand, optimize protein-ligand interactions, or identify potential ligands for a given protein target. In certain embodiments, the invention contemplates the synthesis of the following methotrexate-containing heterodimeric probe:

    专利号:US-12146136-B2
    优先权日:2020-03-26
    标题:Synthesis of modified oligonucleotides with increased stability
    发明人:KHVOROVA ANASTASIA; ROUX LOÃ?C MAURICE RENÉ JEAN; YAMADA KEN
    权利人:UNIV MASSACHUSETTS
    摘要:This disclosure relates to the synthesis of novel modified oligonucleotides. The synthesis of novel phosphoramidites are also 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:US-9605261-B2
    优先权日:2008-09-06
    标 题:RNA synthesis—phosphoramidites for synthetic RNA in the reverse direction, and application in convenient introduction of ligands, chromophores and modifications of synthetic RNA at the 3′-end
    发明人:SRIVASTAVA SURESH C; PANDEY DIVYA; BAJPAI SATYA P; SRIVASTAVA NAVEEN P
    权利人:CHEMGENES CORP
    摘要:The present invention relates to novel phosphoramidites, A-n-bz, C-n-bz, C-n-ac, G-n-ac and U are produced with an HPLC purity of greater than 98% and 31 P NMR purity greater than 99%. A novel process of reverse 5′→3′ directed synthesis of RNA oligomers has been developed and disclosed. Using that method demonstrated high quality RNA synthesis with coupling efficiency approaching 99%.

    专利号:US-2025049714-A1
    优先权日:2021-12-09
    标题 :Synthesis of ester, carbonate, and carbamate-derived novel biodegradable ionizable lipids from methyl ricinoleate or methyl 12-hydroxystearate and its applications
    发明人:ANDERSON DANIEL GRIFFITH; RHYM LUKE HYUNSIK; LI BOWEN; GORDON AKIVA; RAJITH SINGH MANAN; WITTEN JACOB
    权利人:MASSACHUSETTS INST TECHNOLOGY
    摘要:Provided herein are compounds, such as compounds of Formula (I), and pharmaceutically acceptable salts, hydrates, solvates, polymorphs, co-crystals, tautomers, stereoisomers, and isotopically labeled derivatives thereof, and compositions, methods, uses, and kits thereof. The compounds provided herein are lipids useful for delivery of polynucleotides, such as mRNA, for the treatment and/or prevention of various diseases and conditions (e.g., genetic disease, proliferative disease, hematological disease, neurological disease, liver disease, spleen disease, lung disease, painful condition, psychiatric disorder, musculoskeletal disease, a metabolic disorder, inflammatory disease, or autoimmune disease).

    专利号:US-2024226302-A1
    优先权日:2022-12-27
    标题:Biodegradable lipids and formulations for intramuscular, in vitro, and ex vivo transfection of mrna
    发明人:ANDERSON DANIEL GRIFFITH; RUDRA AMAB; GUPTA AKASH; REED KAELAN
    权利人:MASSACHUSETTS INST TECHNOLOGY; CHILDRENS MEDICAL CENTER
    摘要:Provided herein are compounds, such as compounds of Formula (I), and pharmaceutically acceptable salts thereof, and compositions, methods, uses, and kits thereof. The compounds provided herein are lipids useful for delivery of agents, including polynucleotides such as mRNA, for the treatment and/or prevention of various diseases and conditions (e.g., genetic diseases, proliferative diseases, hematological diseases, neurological diseases, liver diseases, spleen diseases, lung diseases, painful conditions, psychiatric disorders, musculoskeletal diseases, metabolic disorders, inflammatory diseases, and autoimmune diseases). Also provided herein are methods of synthesis of compounds of Formulae (I) and (II).
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    主要参考文献

    [参考文献]: Grosso Le, Et Al. Alterations In The Maturation And Structure Of Ribosomal Precursor Rna In Novikoff Hepatoma Cells Induced By 5-Fluorocytidine. Biochemistry. 1984 Jun 5;23(12):2651-6.

    合成参考文献


    摘要:I. Wempen and J.J. Fox. J. Am. Chem. Soc. 86, 2474 (1964).
    参考文献:10.1007/s13277-014-2138-z
    摘要:Kaymaz BT, Cetintaş VB, Aktan C, Kosova B. MicroRNA-520a-5p displays a therapeutic effect upon chronic myelogenous leukemia cells by targeting STAT3 and enhances the anticarcinogenic role of capsaicin. Tumour Biol. 2014 Sep;35(9):8733–42. doi: 10.1007/s13277-014-2138-z.
    参考文献:10.1007/s00294-002-0296-9
    摘要:Kurtz JE, Exinger F, Erbs P, Jund R. The URH1 uridine ribohydrolase of Saccharomyces cerevisiae. Curr Genet. 2002 Jun;41(3):132–41. doi: 10.1007/s00294-002-0296-9.
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