CAS: 932-53-6; 6-Methyl-1,2,4-Triazine-3,5(2H,4H)-Dione

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CAS号615-76-9 6-氮杂-2-硫代胸腺嘧啶 | CAS号2704-30-5 (2E)-2-[(氨基羰基)亚肼基]丙酸 | CAS号13410-30-5 2-(2-Deoxy-beta... | CAS号61959-18-0 2-benzyl-6-meth... | CAS号55846-36-1 6-methyl-1,2,4-...

📜6-氮杂-2-硫代胸腺嘧啶置于双氧水,Sodium Hydroxide,盐酸体系中,用 水 作为反应溶剂,化学反应 0.5H,以79%的收率获得产物6-氮杂胸腺嘧啶
参考文献:6-Aza-2'-脱氧尿苷单磷酸类似物作为胸苷酸合成酶抑制剂以及结核分枝杆菌中胸苷单磷酸激酶的底物或抑制剂的合成和评价
标题:6-Aza-2'-脱氧尿苷单磷酸类似物作为胸苷酸合成酶抑制剂以及结核分枝杆菌中胸苷单磷酸激酶的底物或抑制剂的合成和评价
摘要:6-Aza-2'-Deoxyuridine 5'-Monophosphate 的一系列 5-取代类似物 6-Aza-Dump 已被合成并评估为两种分枝杆菌胸苷酸合酶(即黄素依赖性胸苷酸合酶)的潜在抑制剂,Thyx 和经典的胸苷酸合酶 Thya).用 6-Aza-Dump 1A 中的 N 原子替换天然底物 Dump 的 C(6) 导致衍生物具有弱的 Thyx 抑制活性(50 μm 时抑制率为 33%).在 1A 的 C(5) 处引入烷基和芳基导致抑制活性完全丧失,而衍生物 3 中 3-(辛酰胺基)丙-1-炔基侧链的连接保留了对分枝杆菌 Thyx 的微弱抑制水平. 50 μm 时抑制 40%).合成的衍生物均未显示出对分枝杆菌 Thya 的任何显着抑制活性.这些化合物也被评估为分枝杆菌胸苷单磷酸激酶 (Tmpkmt) 的潜在抑制剂.没有一种衍生物显示出任何显着的 Tmpkmt 抑制.然而,用 N
DOI:10.1002/cbdv.201100285

专利信息

专利号:US-7229797-B1
优先权日:1999-08-20
标 题:Enzymatic synthesis of deoxyribonucleosides
发明人：TISCHER WILHELM; IHLENFELDT HANS-GEORG; BARZU OCTAVIAN; SAKAMOTO HIROSHI; PISTOTNIK ELISABETH; MARLIERE PHILIPPE; POCHET SYLVIE
权利人:PASTEUR INSTITUT
摘要:The present invention relates to a method for the in vitro enzymatic synthesis of deoxyribonucleosides and enzymes suitable for this method.

专利号:US-6624294-B2
优先权日:1999-01-08
标 题:Regioselective synthesis of 2′-O-modified nucleosides
发明人：KAWASAKI ANDREW M; FRASER ALLISTER S; MANOHARAN MUTHIAH; COOK P DAN; PRAKASH THAZHA P
权利人:ISIS PHARMACEUTICALS INC
摘要:Methods for the regioselective alkylation at the 2'-hydroxy position over the 3'-hydroxy position of nucleosides and nucleoside analogs, forming 2'-O-ester modified compounds, are disclosed. Reduction and derivatization of the 2'-O-ester provides 2'-O-modified nucleosides and nucleoside analogs useful for the synthesis of oligomeric compounds having improved hybridization affinity and nuclease resistance.

专利号:US-4849513-A
优先权日:1983-12-20
标 题 :Deoxyribonucleoside phosphoramidites in which an aliphatic amino group is attached to the sugar ring and their use for the preparation of oligonucleotides containing aliphatic amino groups
发明人：SMITH LLOYD M; FUNG STEVEN; KAISER ROBERT J
权利人:CALIFORNIA INST OF TECHN
摘要:The invention consists of compounds and methods for the synthesis of oligonucleotides which contain one or more free aliphatic amino groups attached to the sugar moieties of the nucleoside subunits. The synthetic method is versatile and general, permitting amino groups to be selectively placed at any position on oligonucleotides of any composition or length which is attainable by current DNA synthetic methods. Fluorescent dyes or other detectable moieties may be covalently attached to the amino groups to yield the corresponding modified oligonucleotide.

专利号:US-5118802-A
优先权日:1983-12-20
标 题:DNA-reporter conjugates linked via the 2' or 5'-primary amino group of the 5'-terminal nucleoside
发明人：SMITH LLOYD M; FUNG STEVEN; KAISER JR ROBERT J
权利人:CALIFORNIA INST OF TECHN
摘要:The invention consists of compounds and methods for the synthesis of oligonucleotides which contain one or more free aliphatic amino groups attached to the sugar moieties of the nucleoside subunits. The synthetic method is versatile and general, permitting amino groups to be selectively placed at any position on oligonucleotides of any composition or length which is attainable by current DNA synthetic methods. Fluorescent dyes or other detectable moieties may be covalently attached to the amino groups to yield the corresponding modified oligonucleotide.

专利号:US-5118800-A
优先权日:1983-12-20
标 题 :Oligonucleotides possessing a primary amino group in the terminal nucleotide
发明人：SMITH LLOYD M; FUNG STEVEN; KAISER JR ROBERT J
权利人:CALIFORNIA INST OF TECHN
摘要:The invention consists of compounds and methods for the synthesis of oligonucleotides which contain one or more free aliphatic amino groups attached to the sugar moieties of the nucleoside subunits. The synthetic method is versatile and general, permitting amino groups to be selectively placed at any position on oligonucleotides of any composition or length which is attainable by current DNA synthetic methods. Fluorescent dyes or other detectable moieties may be covalently attached to the amino groups to yield the corresponding modified oligonucleotide.

专利号:US-6277982-B1
优先权日:1999-08-20
标题:Alkylation of alcohols, amines, thiols and their derivatives by cyclic sulfate intermediates
发明人：FRASER ALLISTER S; MANOHARAN MUTHIAH; COOK PHILLIP DAN; JUNG MICHAEL E; KAWASAKI ANDREW M
权利人:ISIS PHARMACEUTICALS INC
摘要:Methods for the alkylation of alcohols, amines and thiols by the use of cyclic sulfates are disclosed. The alkylated sulfates formed are versatile intermediates which may be further elaborated by methods of the invention. In particular, methods for the alkylation of the 2′, 3′ or 5′-hydroxy position of nucleosides and nucleoside analogs with cyclic sulfates to form the 2′, 3′ or 5′-O-alkyl sulfate modified compounds are disclosed. Displacement of the 2′,3′ or 5′-O-sulfate with a nucleophile provides 2′, 3′ or 5′-O-modified nucleosides and nucleoside analogs useful for the synthesis of oligomeric compounds having improved hybridization affinity and nuclease resistance.