CAS: 106941-25-7; ((2-(6-Amino-9H-Purin-9-yl)Ethoxy)Methyl)Phosphonic Acid

相似化合物

147127-19-3 147127-20-6 107021-27-2

上下游产品

CAS号116384-53-3 [[2-(6-氨基-9H-嘌呤... | CAS号142340-94-1 diisopropyl ((2... | CAS号707-99-3 9-(2-羟乙基)腺嘌呤 | CAS号212894-84-3 diethyl ((2-((5... | CAS号185900-69-0 diethyl ((2-(6-... | CAS号66224-66-6 6H-Purin-6-imin... | CAS号107021-27-2 Methyl Ester of... | CAS号31618-90-3 对甲苯磺酰氧甲基膦酸二乙酯 | CAS号159531-21-2 {[2-(6-amino-9H... | CAS号142341-38-6 9-[2-(dichlorop... | CAS号116384-53-3 [[2-(6-氨基-9H-嘌呤... | CAS号142340-99-6 阿德福韦酯 | CAS号323201-04-3 9-[2-({bis[(piv... | CAS号142341-24-0 9-[2-(diphenoxy... | CAS号113884-65-4 2-(6-oxo-3H-pur...

阿德福韦酯置于乙二胺四乙酸,Dl-Dithiothreitol,水,Magnesium Chloride体系中,用 Aq. Buffer 用作溶剂,化学反应 1.0H,反应生成阿德福韦
参考文献:2-取代9-[2-(膦氧基甲氧基)乙基]腺嘌呤(pmea,阿德福韦)的双氨基酸盐前药作为百日咳博德特氏菌腺苷酸环化酶毒素的选择性抑制剂
标题:2-取代9-[2-(膦氧基甲氧基)乙基]腺嘌呤(pmea,阿德福韦)的双氨基酸盐前药作为百日咳博德特氏菌腺苷酸环化酶毒素的选择性抑制剂
摘要:人们迫切需要新型的小分子药物来治疗百日咳博德特氏菌感染,因为百日咳(咳嗽)仍然是世界范围内严重的健康威胁.在这项研究中,设计并合成了一系列以异丙酯双(l-苯丙氨酸)前药形式存在的9-[2-(膦酰基甲氧基)乙基]腺嘌呤的2-取代衍生物(pmea,阿德福韦),并合成了它们的有效抑制剂.百日咳博德特氏菌分离的腺苷酸环化酶毒素(act).该系列由pmea类似物组成,这些pmea类似物在嘌呤部分的c2位置带有直链或支链脂族链或杂原子.具有小的c2取代基的化合物显示出对act的高效力,而没有细胞毒性作用,并且对人腺苷酸环化酶亚型ac1,Ac2和ac5具有非常好的选择性.最有效的act抑制剂发现是2-氟pmea衍生物的双酰胺前体药物(ic 50 = 0.145μ中号).尽管本文报道的双氨基酸盐前药总体上比双(新戊酰氧甲基)前药(阿德福韦酯)具有更低的活性,但它们的毒性和血浆稳定性却很出色.此外,已显示双
Doi:10.1002/cmdc.201500183

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-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.

专利号:US-9334273-B1
优先权日:2014-03-05
标题:Efficient and stereoselective synthesis of 2′-fluoro-6′-methylene-carbocyclic adenosine (FMCA)
发明人：CHU DAVID C K; SINGH UMA S
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) from a readily available starting material (Vince lactam) in fourteen steps. An efficient and practical methodology for stereospecific preparation of a versatile carbocyclic key intermediate, D -2′-fluoro-6′-methylene cyclopentanol by diazotization, elimination, stereoselective epoxidation, fluorination and oxidative reduction of the Vince lactam in twelve steps is also provided.

专利号:US-7582758-B2
优先权日:2004-06-08
标 题:Lewis acid mediated synthesis of cyclic esters
发明人：MARTIN KEVIN V
权利人:METABASIS THERAPEUTICS INC
摘要:Methods for the synthesis of cyclic phosphonic acid diesters from 1,3-diols are described, whereby cyclic phosphonic acid diesters are produced by reacting a chiral 1,3-diol and an activated phosphonic acid in the presence of a Lewis acid.

专利号:US-6818633-B2
优先权日:2001-06-29
标题:Antiviral compounds and methods for synthesis and therapy
发明人：BALZARINI JAN M R; DE CLERCQ ERIK D A; HOLY ANTONIN
权利人:ACAD OF SCIENCE CZECH REPUBLIC; REGA STICHTING
摘要:Novel compounds are provided having formula (I)whereR1, R2, R3, R4, Z, X and * are defined herein. Also provided are antiviral methods for use and processes for synthesis of the compounds of formula (I).

专利号:US-2015376219-A1
优先权日:2014-06-30
标题 :Selective Preparations of Purine Nucleosides and Nucleotides: Reagents and Methods
发明人：ZHONG MINGHONG
权利人:ZHONG MINGHONG
摘要:A process of regiospecific synthesis of N-9 purine nucleoside analogs in either solution or solid phase synthesis is described. The introduction of the sugar moiety or its analogue on to a 6-heteroarylium purine or its mesomeric betaine so that formation of only the N-9 position regioisomers of the purine nucleoside analogs (either D or L enantiomers) is obtained. This regiospecific introduction of the sugar moiety allows the synthesis of purine nucleoside analogs in high yields without formation of the N-7-positional regioisomers, while the 6-heteroaryliums are leaving groups facilitated for nucleophilic displacement. Solid supported 6-heterarylium purine bases can be used for purine based library synthesis and synthesis of nucleotide monophosphates and polyphosphates. Processes for providing novel 6-heteroarylium purines and their corresponding mesomeric betaines for the regiospecific synthesis of N-9 purine nucleoside analogs and nucleotides are described.