A_(2A)腺苷受体拮抗剂中间体与抗结剂合成方法研究  

Synthesis of an important intermediate of antagonists of the human A_(2A) adenosine receptor

作　　者：屠美玲[1] 俞卫平[2] 冯涛[2] 贾继宁[1] 张云[1] 张建庭[1] 

机构地区：[1]浙江工业大学化学工程与材料学院,浙江杭州310014 [2]杭州职业技术学院,浙江杭州310018

出　　处：《浙江大学学报（理学版）》2016年第4期420-425,共6页Journal of Zhejiang University（Science Edition）

摘　　要：基于官能化的三唑并[4,5-d]嘧啶类拮抗剂对人体内A_(2A)腺苷受体拮抗作用的干预治疗,能有效缓解帕金森综合征的临床症状.该类拮抗剂可以提高多巴胺神经元对纹状体多巴胺的敏感度.重点研究了三唑并[4,5-d]嘧啶类拮抗剂合成所需的重要中间体4-氯-1H-[1,2,3]三唑并[d]嘧啶-6-胺的合成、表征及应用.并对该中间体进行活性拼接,制备了含呋喃基的三唑并[4,5-d]嘧啶类拮抗剂8.Antagonism of the human A_（2A） receptor has been implicated as a point of therapeutic intervention in the alleviation of the symptoms associated with Parkinson＇s disease.That is to say,at least in part,this kind of antagonists can improve the sensitivity of the dopaminergic neurons to the residual,and deplete levels of striatal dopamine.Herein,we reported a novel synthesis strategy of an important intermediate（4-chloro-1H-benzo[d][1,2,3]triazol-6-amine）of antagonists of the human A_（2A） adenosine receptor.Additionally,we had also prepared the adenosine receptor 8.

关 键 词：帕金森综合征 A2A腺苷受体拮抗剂 合成 

分 类 号：TQ46[化学工程—制药化工]