CAS: 5451-40-1; 2,6-Dichloropurine

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CAS号69-89-6 黄嘌呤 | CAS号10310-21-1 2-氨基-6-氯嘌呤 | CAS号110-46-3 亚硝酸异戊酯 | CAS号65996-50-1 1H-吡咯并[2,3-d]嘧啶... | CAS号5167-14-6 次黄嘌呤 1-氧化物 | CAS号700-02-7 腺嘌呤-N1-氧化物 | CAS号97965-44-1 N-(9-acetyl-6-c... | CAS号73-40-5 鸟嘌呤 | CAS号149948-29-8 N'-(6-chloro-7H... | CAS号190962-00-6 6-chloro-2-form... | CAS号1056016-74-0 2-氯-9-(1-甲基乙基)-... | CAS号4291-63-8 克拉利宾 | CAS号37390-66-2 2,6-二氯嘌呤-2'-脱氧核苷 | CAS号5437-25-2 2,6-二巯基嘌呤 | CAS号59587-07-4 2-Azidoadenosine | CAS号39639-47-9 N-苄基-2-氯-9H-嘌呤-6-胺 | CAS号20419-68-5 2,6-二氯-9-(四氢-2H... | CAS号186692-44-4 2-[[9-(1-甲基乙基)-... | CAS号186692-41-1 N-苄基-2-氯-9-异丙基-... | CAS号1928-79-6 2,6-bis(1-piper...

鸟嘌呤置于盐酸,Sodium Hydroxide,Zinc(II) Chloride,三氯氧磷体系中,用 水,1,2-二氯乙烷 作为反应溶剂,化学反应 13.5H,反应生成 2,6-二氯嘌呤
参考文献:设计,合成和评估4-氨基喹啉-嘌呤杂种作为潜在的抗疟原虫药物
标题:设计,合成和评估4-氨基喹啉-嘌呤杂种作为潜在的抗疟原虫药物
摘要:一种新颖的一系列4-氨基喹啉嘌呤杂交合成并评价了它们对的cq-敏感和cq抗性株抗疟原虫活性p.恶性肿瘤.设想将4-氨基喹啉药效团(靶向疟原虫的血红素-解毒途径)与嘌呤功能性(靶向血浆hg(x)prt酶)连接将产生具有增强效力的杂合抗血浆剂.将合成的杂种显示针对两者的敏感和抗性菌株的非常好抗疟原虫活性p.与参考药物cq(ic)相比,具有更好的六倍活性(化合物10I,Ic 50:0.08μm)的恶性疟原虫50:0.5μm)抗性菌株.还检查了合成的化合物对哺乳动物细胞的细胞毒性,除了二十个合成的杂合物中的两种化合物外,其他所有化合物在至多11.86μm的浓度下均无细胞毒性.进行了机制血红素结合研究,以确定合成分子的作用机理,并观测到非常好的结合相互作用.计算对接研究表明,最活跃的杂种很好地对接在hgprt蛋白的结合位点内.在计算机模拟adme中,对最活跃的杂种的预测表明,这些化合物具有非常好的药代动力学行为.
DOI:10.1016/j.Ejmech.2016.11.057

专利信息

专利号:EP-1709057-B1
优先权日:2004-01-21
标 题:Synthesis of spongosine
发明人：OUZMAN JACQUELINE VALERIE ANNE
权利人:CAMBRIDGE BIOTECHNOLOGY LTD
摘要:Reaction of 1-O-acetyl-2,3,5-tri-O-benzoyl-β-D-ribofuranose with 2-methoxyadenine to form 9-(2′,3′,5′-tri-O-benzoyl-β-D-ribofuranosyl)-2-methoxyadenine, then deprotection of the 9-(2′,3′,5′-tri-O-benzoyl-β-D-ribofuranosyl)-2-methoxyadenine to form spongosine is described. Synthesis of intermediates for use in the synthesis of spongosine is also described.

专利号:US-7229797-B1
优先权日:1999-08-20
标 题:Enzymatic synthesis of deoxyribonucleosides
发明人：TISCHER WILHELM; IHLENFELDT HANS-GEORG; BARZU OCTAVIAN; SAKAMOTO HIROSHI; PISTOTNIK ELISABETH; MARLIERE PHILIPPE; POCHET SYLVIE
权利人:PASTEUR INSTITUT
摘要:The present invention relates to a method for the in vitro enzymatic synthesis of deoxyribonucleosides and enzymes suitable for this method.

专利号:US-4849513-A
优先权日:1983-12-20
标 题 :Deoxyribonucleoside phosphoramidites in which an aliphatic amino group is attached to the sugar ring and their use for the preparation of oligonucleotides containing aliphatic amino groups
发明人：SMITH LLOYD M; FUNG STEVEN; KAISER ROBERT J
权利人:CALIFORNIA INST OF TECHN
摘要:The invention consists of compounds and methods for the synthesis of oligonucleotides which contain one or more free aliphatic amino groups attached to the sugar moieties of the nucleoside subunits. The synthetic method is versatile and general, permitting amino groups to be selectively placed at any position on oligonucleotides of any composition or length which is attainable by current DNA synthetic methods. Fluorescent dyes or other detectable moieties may be covalently attached to the amino groups to yield the corresponding modified oligonucleotide.

专利号:US-5118802-A
优先权日:1983-12-20
标 题:DNA-reporter conjugates linked via the 2' or 5'-primary amino group of the 5'-terminal nucleoside
发明人：SMITH LLOYD M; FUNG STEVEN; KAISER JR ROBERT J
权利人:CALIFORNIA INST OF TECHN
摘要:The invention consists of compounds and methods for the synthesis of oligonucleotides which contain one or more free aliphatic amino groups attached to the sugar moieties of the nucleoside subunits. The synthetic method is versatile and general, permitting amino groups to be selectively placed at any position on oligonucleotides of any composition or length which is attainable by current DNA synthetic methods. Fluorescent dyes or other detectable moieties may be covalently attached to the amino groups to yield the corresponding modified oligonucleotide.

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.

专利号:US-7855285-B2
优先权日:2005-06-14
标 题:Methods for selective N-9 glycosylation of purines
发明人：ROBINS MORRIS J; ZHONG MINGHONG
权利人:UNIV BRIGHAM YOUNG
摘要:A process for providing regiospecific and highly stereoselective synthesis of 9-β anomeric purine nucleoside analogs is described. The introduction of the sugar moiety on to 6-(azolyl)-substituted purine bases is performed so that highly stereoselective formation of the β anomers of only the 9 position regioisomers of the purine nucleoside analogs (either D or L enantiomers) is obtained. This regiospecific and stereoselective introduction of the sugar moiety allows the synthesis of nucleoside analogs, and in particular 2′-deoxy, 3′-deoxy, 2′-deoxy-2′-halo-arabino and 2′,3′-dideoxy-2′-halo-threo purine nucleoside analogs, in high yields without formation of the 7-positional regioisomers. Processes for providing novel 6-(azolyl)purines for the regiospecific and highly stereoselective synthesis of 9-β anomeric purine nucleoside analogs are described. The compounds are drugs or intermediates to drugs.