CAS: 145416-34-8; (-)-(2S,5S)-5-Fluoro-1-(2-(Hydroxymethyl)-1,3-Oxathiolan-5-yl)Cytosine

上下游产品

Trans-2-Benzoyloxymethyl-5-(N'4-Acetyl-5'-Fluorocytosin-1'-yl)-1,3-Oxathiolane

📜(-)-(2S,5S)-5-Fluoro-1-<2-<<(Tert-Butyldiphenylsilyl)Oxy>Methyl>-1,3-Oxathiolan-5-Yl>-N4-Benzoylcytosine置于四丁基氟化铵,氨体系中,用 四氢呋喃,甲醇 用作溶剂,化学反应 1.0H,反应生成2-表-恩曲他滨
参考文献:β-D-(2S,5R)-和α-D-(2S,5S)-1,3-氧杂硫杂环戊基核苷作为潜在抗hiv药物的结构活性关系.
标题:β-D-(2S,5R)-和α-D-(2S,5S)-1,3-氧杂硫杂环戊基核苷作为潜在抗hiv药物的结构活性关系.
摘要:合成了具有天然核苷构型的β-D-(2S,5R)-和α-D-(2S,5S)-1,3-氧杂硫基丙基嘧啶和-嘌呤核苷,并针对人外周血单核(pbm)中的hiv-1进行了评估) 细胞.由d-甘露糖或d-半乳糖合成了用于合成各种核苷的关键中间体14.乙酸盐14与胸腺嘧啶,尿嘧啶,胞嘧啶和5-取代的尿嘧啶和胞嘧啶的缩合得到各种嘧啶核苷.乙酸酯14也与6-氯嘌呤和6-氯-2-氟嘌呤缩合,将其转化为各种嘌呤核苷.就胸腺嘧啶,尿嘧啶和5-取代的尿嘧啶衍生物而言,除5-氟尿嘧啶(α-异构体)衍生物55以外,大多数化合物均未表现出任何显着的抗hiv活性.在5-取代的胞嘧啶类似物中,发现5-溴胞嘧啶衍生物(β-异构体)68是最有效的抗hiv药物.在嘌呤衍生物的情况下,肌苷类似物(β-异构体)78被发现是6-取代嘌呤中最有效的抗hiv药物,而2-氨基-6-氯嘌呤衍生物(β-异构体)90显示最多. 2,6-二取代嘌呤系
Doi:10.1021/jm00070A006

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-6143748-A
优先权日:1995-03-31
标题:Process for synthesis of nucleoside analogues
发明人：SAMANO MIRNA C; SAMANO VICENTE; GOODYEAR MICHAEL DAVID
权利人:GLAXO WELLCOME INC
摘要:The present invention is concerned with a process for the preparation of antiviral 1,3-oxathiolane nucleosides comprising an intramolecular glycosylation reaction to produce exclusively the β-diastereomer, and intermediates useful in the process.

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