CAS: 15763-11-8; (2R,3R,4S,5R)-2-(6-Amino-2-Hydrazinyl-9H-Purin-9-yl)-5-(Hydroxymethyl)Tetrahydrofuran-3,4-Diol

相似化合物

58-61-7 3080-29-3 5536-17-4

上下游产品

2-Chloroadenosine 2',3',5'-tri-O-acetyl-2-chloroadenosine 2-iodoadenosine 2-chloro-6-methoxy-purine riboside

📜鸟苷置于4-二甲氨基吡啶,亚硝酸苄基三乙基铵,Hydrazine Hydrate,二甲基十二/十四烷基叔胺,乙醇,四乙基氯化铵,氨,N,N-二甲基苯胺,乙酰氯,三氯氧磷体系中,用 二氯甲烷,乙腈 用作溶剂,化学反应 4.0H,反应生成2-肼基腺苷
参考文献:2位取代的α,β-亚甲基adp衍生物:具有可变结合模式的强效竞争性ecto-5'-核苷酸酶(cd73)抑制剂.
标题:2位取代的α,β-亚甲基adp衍生物:具有可变结合模式的强效竞争性ecto-5'-核苷酸酶(cd73)抑制剂.
摘要:Cd73抑制剂是用于癌症(免疫)治疗的有前途的药物.在这里,我们介绍了合成,结构-活性关系,和竞争性cd73抑制剂α,β-亚甲基-Adp(aopcp)取代2位的新型衍生物的共晶体结构.小极性或亲脂性残基增加了效力,2-碘-和2-氯腺苷-5'-O-[(膦酰基甲基)膦酸](15,16)是对人cd73的ki值为3-的最有效抑制剂6 Nm.取决于2-取代基的大小和性质,通过x射线晶体学观测到可变的结合模式.取决于结合模式,发现了较大的物种差异,例如,2-哌嗪基-Aopcp(21)与人cd73相比,对大鼠cd73的效力低> 12倍.这项研究表明,只需将一个小的取代基引入aopcp的2位即可实现高cd73抑制力,而无需额外的大体积n6-取代基.此外,它为竞争性cd73抑制剂的结合模式提供了宝贵的见解,为药物开发提供了极好的基础.
Doi:10.1021/acs.Jmedchem.9B01611

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:US-RE47301-E
优先权日:2006-02-03
标题 :Process for preparing an A2A-adenosine receptor agonist and its polymorphs
发明人：ZABLOCKI JEFF; ELZEIN ELFATIH; SEEMAYER ROBERT; LEMONS TRAVIS
权利人:GILEAD SCIENCES INC
摘要:Disclosed is a synthesis suitable for large scale manufacture of an A 2A -adenosine receptor agonist, and also relates to polymorphs of that compound, and to methods of isolating a specific polymorph.