CAS: 134680-32-3; 4-Amino-1-((2S,5R)-2-(Hydroxymethyl)-1,3-Oxathiolan-5-yl)Pyrimidin-2(1H)-One

相似化合物

134678-17-4 143491-57-0 136891-12-8

上下游产品

methyl>-5-(cytosin-1'-yl)-1,3-oxathiolanecis-2-(tert-butyldiphenylsilyl)oxymethyl-5-(cytosin-1'-yl)-1,3-oxathiolane cis-2-benzoyloxymethyl-5-(N'4-acetylcytosin-1'-yl)-1,3-oxathiolane cis/trans-2-benzoyloxymethyl-5-(cytosin-1'-yl)-1,3-oxathiolane L-menthyl 5-cytosin-1-yl-1,3-oxathiolane-2-carboxylatemethyl>-5-(cytosin-1'-yl)-1,3-oxathiolanecis-2-(tert-butyldiphenylsilyl)oxymethyl-5-(cytosin-1'-yl)-1,3-oxathiolane

📜(+)-(2S,5R)-1-<2-<<(Tert-Butyldiphenylsilyl)Oxy>Methyl>-1,3-Oxathiolan-5-Yl>-Cystosine置于四丁基氟化铵体系中,用 四氢呋喃 用作溶剂,以75%的收率获得ent-拉米夫定
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:WO-2022256490-A9
优先权日:2021-06-03
标题:Improved synthesis of phosphoramidates for the treatment of hepatitis b virus
发明人：LOCKWOOD MARK
权利人:ANTIOS THERAPEUTICS INC
摘要:The synthesis of phosphoramidate prodrugs useful in the treatment of viral infections is disclosed. Specifically, an improved synthesis of phosphoramidate nucleotides useful in the treatment of Hepatitis B virus is disclosed.

专利号:US-2003162992-A1
优先权日:2001-12-14
标 题 :Preparation of intermediates useful in the synthesis of antiviral nucleosides
发明人：WATANABE KYOICHI A; DU JINFA
摘要:The present invention is an efficient process for the manufacture of α-acyloxyacetaldehyde, a key intermediate in the synthesis of 1,3-oxathiolane and 1,3-dioxolane nucleosides.

专利号:US-9206209-B2
优先权日:2010-10-19
标 题:Nucleotide analogue, method of synthesis of nucleotide analogue, use of nucleotide analogue, antiviral pro-nucleotide, pharmaceutical composition
发明人：KRASZEWSKI ADAM; ROMANOWSKA JOANNA; SOBKOWSKI MICHAL; SZYMANSKA-MICHALAK AGNIESZKA; STAWINSKI JACEK; BORYSKI JERZY; LIPNIACKI ANDRZEJ; PIASEK ANDRZEJ
权利人:KRASZEWSKI ADAM; ROMANOWSKA JOANNA; SOBKOWSKI MICHAL; SZYMANSKA-MICHALAK AGNIESZKA; STAWINSKI JACEK; BORYSKI JERZY; LIPNIACKI ANDRZEJ; PIASEK ANDRZEJ; INST CHEMII BIOORG PAN; NARODOWY INST LEKOW
摘要:An exemplary emboidment is related to a pharmaceutical composition of the class of nucleotide analogues and antiviral pro-nucleotides useful in partial or complete inhibition of human immunodeficiency virus (HIV). An exemplary embodiment is expressed in the formula (XVI): n nwhere X stands for N 3 and B stands for thymidine-1-yl, or X stands for H and B stands for uracil-1-yl or adenin-1-yl or hypoxanthin-1-yl.A method of synthesis of the nucleotide analogue using a phosphorylating agent for synthesis of the nucleotide analogue is 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-8304540-B2
优先权日:2007-05-18
标题:Process for stereoselective synthesis of lamivudine
发明人：LI JINLIANG; LV FENG
权利人:LI JINLIANG; LV FENG; SHANGHAI DESANO PHARMACEUTICAL HOLDING CO LTD
摘要:The present invention discloses a process for stereoselective synthesis of Lamivudine comprising the following steps: (a) performing a glycosylation reaction between the compound of formula (I) and cytosine or protected cytosine, and separating the reaction product by recrystallization to obtain the intermediate of formula (II); and (b) deprotecting the intermediate of formula (II) to obtain Lamivudine.

专利号:US-10995093-B2
优先权日:2016-04-07
标 题 :Synthesis of 2′-fluoro-6′-methylene-carbocyclic adenosine (FMCA) and 2′-fluoro-6′methylene-carbocyclic guanosine (FMCG)
发明人：CHU CHUNG K; MULAMOOTTTIL VARUGHESE ALEXANDER; MISHRA RAM C; SINGH UMA SHARAN
权利人:UNIV GEORGIA
摘要:The invention provides a new convergent approach for the synthesis of 2′-fluoro-6′-methylene-carbocyclic adenosine (FMCA) and 2′-fluoro-6′-methylene-carbocyclic guanosine (FMCG) from a readily available starting material in eight steps. An efficient and practical methodology for stereospecific preparation of a versatile carbocyclic key intermediate, (1S,3R, 4R)-3-tert-butoxy-4-(tert-butoxymethyl)-2-fluoro-5-methylenecyclopentanol (compound 8 of scheme 1A or a) in only six (6) steps is also provided. Prodrugs of these compounds are also prepared.