瑞加德松的合成  

Synthesis of Regadenoson

作　　者：罗海荣 柴健 顾荣领 俞旭峰 

机构地区：[1]浙江海正药业股份有限公司,浙江台州310008

出　　处：《中国医药工业杂志》2014年第8期705-707,共3页Chinese Journal of Pharmaceuticals

摘　　要：2-氯腺嘌呤与水合肼反应得2-肼基腺嘌呤,与2-甲酰基-3-氧代丙酸乙酯成环得1-(6-氨基-9H-嘌呤-2-基)-1H-吡唑-4-羧酸乙酯,经甲胺化所得产物与1,2,3,5-四-O-乙酰基-β-D-核糖在三氟甲磺酸三甲基硅酯(TMSOTf)作用下反应,继而经氢氧化钠水解得瑞加德松,总收率约43%,纯度98.6%。Regadenoson was synthesized by reaction from 2-chloroadenine and hydrazine hydrate to give 2-hydrazinoadenine, which was subjected to cyclization with ethyl 2-formyl-3-oxopropionate, amination with methylamine, glycosidation with 1,2,3,5-tetra-O-acetate-β-D-ribofuranose in the presence of trimethylsilyl triflate （TMSOTf）, followed by hydrolysis with sodium hydroxide. The overall yield was about 43 % with 98.6 % purity.

关 键 词：瑞加德松 A2A腺苷受体激动剂 冠状血管扩张剂 合成 

分 类 号：R981[医药卫生—药品]