An Alternative Approach to Synthesize Sildenafil via Improved Copper-Catalyzed Cyclization
Abdullajon Odilov,
Xudong Gong,
Hongjian Qin
et al.
Abstract:A facile synthetic pathway for sildenafil has been developed. This approach is characterized by a ligand-free Ullmanntype copper-catalyzed coupling reaction to construct sildenafil and its derivative, pyrrazolo [4,3-d]pyrimidin-7-one ring, with yields of 79% and 82%, respectively, in a convergent fashion by connecting key building blocks halo-pyrazole moiety 16c with 2-ethoxybenzamidine and 2-ethoxy-5-[(4-methylpiperazin-1-yl)sulfonyl]benzamidine in a one-pot reaction. Thus, this approach circumvents the need … Show more
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