Objective: To improve the process for the synthesis of regadenoson and its quality.Methods: Regadenoson was synthesized from 2-chloroadenosine via etherification with tert-butyldimethylchlorosilane and reacted with hydrazine hydrate to give 2′,3′,5′-tri-(tert-butyldimethylsiyl)oxy-2-hydrazinyl adenosine, which was cyclized with Et 2-formyl-3-oxopropanoate, and finally the protecting groups were removed.Results: The purity and yield of regadenoson were improved up to 99.0% and 47.2%, resp.Conclusion: The improved process can be easily operated with high yield and quality, which is suitable to industrial production