CAS: 35109-88-7; (2R,3R,4S,5R)-2-(6-Amino-2-Iodo-9H-Purin-9-yl)-5-(Hydroxymethyl)Tetrahydrofuran-3,4-Diol

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鸟苷置于吡啶,亚硝酸特丁酯,二碘甲烷,氨,四甲基氯化铵,N,N-二甲基苯胺,三氯氧磷体系中,用 N,N-二甲基甲酰胺,乙腈 用作溶剂,化学反应 25.4H,反应生成2-碘腺苷
参考文献:嘌呤核苷类似物的合成,表征和生物学评价
标题:嘌呤核苷类似物的合成,表征和生物学评价
摘要:我们提出一个方便的途径为c6氨基c5'-合成ñ环丙基甲酰氨基c2-炔基化的嘌呤核苷类似物11A-克经由sonogashira偶联反应.使用市售试剂,九步合成易于进行.化合物9被用作合成类似物11A-G的关键中间体.合成中间体和终产物通过ir,1 H NMR,13 C NMR和质量进行了适当表征.修饰后的核苷类似物11A-G在体外进行了评估.对mda-Mb-231和caco-2细胞系的抗癌活性.筛选数据表明,与标准药物阿霉素相比,化合物11B和11E对mda-Mb-231的有效ic 50值分别为7.9,6.8 µg / Ml和对caco-2的有效ic 50值分别为7.5,8.3 µg / Ml.这些新型衍生物的抗癌特性.
Doi:10.1016/j.Tetlet.2017.09.041

专利信息

专利号:US-8859522-B2
优先权日:2011-04-27
标题:Processes for the preparation of regadenoson and a new crystalline form thereof
发明人：WOOLDRIDGE LUZVIMINDA T; MA CHUN; NADJI SOURENA
权利人:WOOLDRIDGE LUZVIMINDA T; MA CHUN; NADJI SOURENA; RELIABLE BIOPHARMACEUTICAL CORP
摘要:This disclosure relates to an improved process for the preparation of regadenoson, pharmaceutically acceptable salts thereof, and hydrates thereof, and for the preparation of intermediates useful in the synthesis of regadenoson. The disclosure also relates to a new crystalline form of regadenoson. Processes for the preparation of the crystalline form, compositions containing the crystalline form, and methods of use thereof are also described.

专利号:US-9771390-B2
优先权日:2013-12-10
标题:Process for the preparation of regadenoson
发明人：ZHANG XIAOHENG; MEI LIJUN
权利人:SCINOPHARM TAIWAN LTD
摘要:The present invention provides novel processes for the preparation of regadenoson having the formula (I). In some embodiments, the intermediates for the synthesis of regadenoson are also provided.

专利号:EP-0429681-A1
优先权日:1989-06-20
标 题 :Intermediate for 2-alkynyladenosine synthesis, production of said intermediate, production of 2-alkynyladenosine from said intermediate, and stable 2-alkynyladenosine derivative

专利号:WO-9015812-A1
优先权日:1989-06-20
标题:Intermediate for 2-alkynyladenosine synthesis, production of said intermediate, production of 2-alkynyladenosine from said intermediate, and stable 2-alkynyladenosine derivative

专利号:EP-0429681-B1
优先权日:1989-06-20
标题 :Intermediate for 2-alkynyladenosine synthesis, production of said intermediate, production of 2-alkynyladenosine from said intermediate, and stable 2-alkynyladenosine derivative