📜4-氯-2-甲硫基嘧啶-5-羧酸乙酯置于水,Sodium Hydroxide体系中,用 乙醇 作为反应溶剂,化学反应 2.0H,以75%的收率获得产物4-羟基-2-(甲硫基)嘧啶-5-羧酸 参考文献: Heterocyclic Compounds And Uses Thereof[fr] Composés Hétérocycliques Et Leurs Utilisations 标题: Heterocyclic Compounds And Uses Thereof[fr] Composés Hétérocycliques Et Leurs Utilisations 摘要:提供了一种作为weel抑制剂的杂环化合物.这些化合物可能用作治疗疾病的治疗剂,特别是在肿瘤学中可能具有特殊用途.
专利号:US-2004033967-A1 优先权日:2000-08-30 标题:Alkylated hexitol nucleoside analogues and oligomers thereof 发明人:VAN AERSCHOT ARTHUR; HERDEWIJN PIET 摘要:The present invention is directed to nucleoside analogues with as substitute for the sugar part a 1,5-anhydrohexitol moiety, doexygenated and substituted with a nucleobase at the 2-position, of which the hexitorl ring is further substituted with at least one alkoxy substituent at the 3-position or at the 1-position, and to oligonucleotides wherein at least some of the nucleotides are part of the afore mentioned hexitol nucleoside analogues and exhibit sequence-specific hydridization to complementary sequences of nucleic acids, and maintaining or improving the hybridisation strength. The invention further relates to nucleoside analogues with a 1,5-anhydrohexitol moiety as the sugar part, deoxygenated and substituted with a nucleobase at the 2-position, of which the hexitol ring is substituted with a methoxy substituent at the 1-position, having at the same time either a hydroxy or an alkoxy group at the 3-position, or having a 3-deoxygenated position. The inclusion of one or more of the afore mentioned hexitol nucleoside analogues in oligonucleotides provides, inter alia, either for improved binding or for maintained binding of these oligonucleotides to a complementary strand. This invention further relates to the chemical synthesis of these oligomers which are useful diagnostics, therapeutics and as research agents.
参考文献:10.1021/acs.jmedchem.1c00605 摘要:Nowak RP, Tumber A, Hendrix E, Ansari MSZ, Sabatino M, Antonini L, Andrijes R, Salah E, Mautone N, Pellegrini FR, Simelis K, Kawamura A, Johansson C, Passeri D, Pellicciari R, Ciogli A, Del Bufalo D, Ragno R, Coleman ML, Trisciuoglio D, Mai A, Oppermann U, Schofield CJ, Rotili D. First-in-Class Inhibitors of the Ribosomal Oxygenase MINA53. J. Med. Chem. 2021 Nov 29;64(23):17031–50. doi: 10.1021/acs.jmedchem.1c00605.