CAS: 73-03-0; (2R,3R,5S)-2-(6-Amino-9H-Purin-9-yl)-5-(Hydroxymethyl)Tetrahydrofuran-3-Ol

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腺苷置于吡啶,偶氮二异丁腈,四丁基氟化铵,三正丁基氢锡体系中,用 四氢呋喃,N,N-二甲基甲酰胺,甲苯 作为反应溶剂,化学反应生成 虫草素
参考文献:甲硫酰基和异亮氨酰氨基磺酸的腺苷酸的脱氧核糖基类似物,作为甲硫酰基-Trna和异亮氨酰-Trna合成酶的抑制剂.
标题:甲硫酰基和异亮氨酰氨基磺酸的腺苷酸的脱氧核糖基类似物,作为甲硫酰基-Trna和异亮氨酰-Trna合成酶的抑制剂.
摘要:研发了异亮氨酰和甲硫氨酸氨基磺酸腺苷酸的2'-脱氧,3'-脱氧和2',3'-二脱氧核糖基替代物,以鉴定核糖基团对抑制大肠杆菌甲硫氨酸-Trna(mrs)和异亮氨酰-Trna(irs)合成酶.具有大肠杆菌mrs晶体结构的2',3'-二脱氧核糖基met-Nhso2-Amp(9)的分子模型表明,核糖之间缺少两个氢键可弥补核糖上两个羟基的缺乏环氧和his24,导致活性降低较小.
DOI:10.1016/j.Bmcl.2005.05.035

专利信息

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-2020239921-A1
优先权日:2016-02-03
标 题 :Chemoenzymatic synthesis of s-nucleosyl amino acids (sna), analogs of s-adenosyl-l-methionine and s-adenosyl-l- homocysteine and uses thereof
发明人：BURGOS EMMANUEL SEBASTIEN; SHECHTER DAVID
权利人:ALBERT EINSTEIN COLLEGE MEDICINE
摘要:Disclosed are methods for chemoenzymatic synthesis of S-Nucleosyl Amino acid probes (SNA), analogs of S-adeno-syl-L-methionine and S-adenosyl-L-homo-cysteine, analogs synthesized by the methods, and uses thereof.

专利号:US-6884880-B2
优先权日:2002-08-21
标 题:Process for the preparation of 9-β-anomeric nucleoside analogs
发明人：GUPTA PRANAB K; MUNK STEPHEN A
权利人:ASH STEVENS INC
摘要:A process for substantially enhancing the regio and stereoselective synthesis of 9-β-anomeric nucleoside analogs is described. The introduction of the sugar moiety onto a 6-substituted purine base was preformed so that only the 9-β-D- or L-purine nucleoside analogs were obtained. This regio and stereoselective introduction of the sugar moiety allows the synthesis of nucleoside analogs and in particular 2′-deoxy, 3′-deoxy, 2′-deoxy-2′-β-fluoro and 2′,3′-dideoxy-2′-β-fluoro purine nucleoside analogs in high yield without virtually any formation of the 7-positional isomers. The compounds are drugs or intermediates to drugs.

专利号:US-2005080260-A1
优先权日:2003-04-22
标 题 :Preparation of prodrugs for selective drug delivery
发明人：MILLS RANDELL L; WU GUO-ZHANG
摘要:Synthesis of a chemical compound having the formula A-B-C that may serve for applications such as drug delivery where A is a chemiluminescent, moiety, B is a photochromic moiety, and C is a biologically active moiety where A-B-C may serve as a prodrug. Novel synthetic methods of the present invention to form the prodrug comprised the steps of (1) forming a benzophenone, (2) forming a diaryl ethylene, (3) attaching a phthalimide moiety to at least one of the aryl groups of the ethylene to form a phthalimide-ethylene conjugate, (4) condensing two ethylene-phthalimide conjugates to form a phthalimide-pentadiene conjugate, (5) converting the phthalimide to the phthalhydrazide by reaction with hydrazine to form a carrier compound according to the present invention, and (6) reacting the carrier compound with an nucleophilic moiety of the drug to form the corresponding prodrug. Alternatively the carrier can be prepared by using the halo-substituted diaryl ethylene to make the corresponding cationic leuco dye-like compound with known methods. The cationic compound then is protected by reacting with a nucleophile and coupled with the aminophathalimide by palladium-catalyzed amination to form the protected phthalimide-pentadiene conjugate. The latter is refluxed with hydrazine to convert its phthalimide to the phthalhydrazide and acidified to give the carrier. An additional aspect of the present invention relates to the use of these compounds as antiviral agents for the treatment of viral infections such as HIV and as anticancer agents for the treatment of cancers such as bowel, lung, and breast cancer.

专利号:US-11897913-B2
优先权日:2017-06-14
标 题:Synthesis of 3′-deoxyadenosine-5′-O-[phenyl(benzyloxy-L-alaninyl)]phosphate (NUC-738)

专利号:US-2020239500-A1
优先权日:2018-04-04
标 题 :Compositions and Methods for Synthesis of Phosphorylated Molecules