CAS: 25526-93-6; 1-((2R,4S,5R)-4-Fluoro-5-(Hydroxymethyl)Tetrahydrofuran-2-yl)-5-Methylpyrimidine-2,4(1H,3H)-Dione

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1-(2,3-二脱氧-3-氟-5-O-三苯甲基呋喃戊糖基)-5-甲基-2,4(1H,3H)-嘧啶二酮置于对甲苯磺酸体系中,用 甲醇,氯仿 用作溶剂,化学反应 0.33H,以64%的收率获得3'-脱氧-3-氟胸苷
参考文献:3'-氟-3'-脱氧胸腺嘧啶核苷的合成及其18 F-放射性标记的研究,作为无创性监测抗艾滋病药物生物分布的示踪剂
标题:3'-氟-3'-脱氧胸腺嘧啶核苷的合成及其18 F-放射性标记的研究,作为无创性监测抗艾滋病药物生物分布的示踪剂
摘要:3'-叠氮基胸苷(azt)的氟化类似物3'-Fluoro-3'-脱氧胸苷(fdt)对hiv病毒更具活性,但比azt毒性更大.由于它具有氟原子,因此可以用18 F标记,以监测该药物的生物分布和靶向性.已经开发出适用于18 F标记的fdt的新合成方法.在用三苯甲基保护5'-羟基后,将3'-羟基用lyxo构型的甲磺酰基取代.用18 F氟化钾和crown-18醚处理可得到18 F标记的氟代衍生物,在去三苯甲基化后可得到18 Ff Fdt具有7%的标记效率.这是首次报道使用氟化钾合成3'-氟-5'-O-三苯甲基脱氧胸苷并制备其18 F标记的类似物.在中间体化合物中掺入18 F并分离终产物所需的时间相当短(大约2小时),这将有足够的时间对这种短寿命的放射性核素进行生物学研究.
Doi:10.1016/s0022-1139(00)82356-8

专利信息

专利号:US-7122693-B2
优先权日:1988-04-11
标题 :Acetaldehyde acetal compounds, their synthesis, and uses thereof
发明人：BELLEAU EXECUTRIX OF ESTATE PI; DIXIT DILIP M; NGUYEN-BA NGHE
权利人:SHIRE BIOCHEM INC
摘要:The acetaldehyde compounds, 2-thiobenzoylacetaldehyde diethylacetal, 2-benzoyloxyacetaldehyde bis(2-methoxyethyl)acetal, 2-hydroxyacetaldehyde bis( 2-methoxyethyl)acetal, 2-thiobenzoylacetaldehyde bis(2-methoxy-ethyl)acetal, and 2-thioacetaldehyde bis(2-methoxyethyl)acetal, are useful as intermediates in the synthesis of substituted 1,3-oxathiolanes and substituted 1,3-dioxolanes.

专利号:US-2003087918-A1
优先权日:1988-04-11
标题 :Synthesis of substituted 1,3-dioxolanes and substituted 1,3-oxathiolanes with antiviral properties

专利号:US-7145000-B2
优先权日:2001-08-23
标题 :Markable compounds for easy synthesis of 3'-[18F] fluoro-3'-deoxynucleotides, and method for their production
发明人：EISENBARTH JOSEPH ANTONIUS MAR; MARTIN STEFAN JOHANNES; WAGNER-UTERMANN ULRIKE; EISENHUT MICHAEL
权利人:DEUTSCHES KREBSFORSCH
摘要:What is described are compounds n n n n n n n n n n n n wherein R represents Br, I or R 1 —SO 3 , where R 1 is an unsubstituted or substituted C 1 –C 5 -alkyl group, or an unsubstituted or substituted phenyl group; n X is O or NR″, where R″ is a usual protective group for N; and n R′ represents hydrogen, a halogen, such as F, Cl, and Br, a substituted or unsubstituted C 1 –C 7 -alkyl group, such as methyl and ethyl, a substituted or unsubstituted C 2 –C 7 -alkenyl group, or a substituted or unsubstituted C 2 –C 7 -alkynyl group.