Synthesis of pyrazolopyrimidinones as sildenafil derivatives and sclerotigenin

ABSTRACT

A series of novel pyrazolo pyrimidinone derivatives (3(a–d), 4(a–d), and 6(a–d)) was synthesized from various pyrazolo amides (2a–d) which are synthesized by the reaction between ethyl 5-amino-3-methyl-1-phenyl-1H-pyrazole-4-carboxylate (1) and various lithium amides. In addition, we also described the synthesis of sclerotigenin drug molecule which has quinazoline moiety from simple 2-nitro benzoic acid with high yields.

GRAPHICAL ABSTRACT

KEYWORDS:

• n-Heteropolycycle
• pyrazolopyrimidinone
• quinazolinone
• sildenafil

Additional information

Funding

Financial support was provided by a grant from the National Research Foundation of Korea (NRF-2014R1A5A1011165) funded by the Korean Government, through the Center for New Directions in Organic Synthesis.