Novel Dual Use of Formamide-POCl₃ Mixture for the Efficient, One-Pot Synthesis of Condensed 2H-Pyrimidin-4-amine Libraries Under Microwave Irradiation

Abstract

The novel dual use of formamide-POCl₃ mixture for the incorporation of a C-N fragment to form the pyrimidine nucleus and its subsequent chlorination in an efficient, one-pot synthesis of potentially bioactive condensed 2H-pyrimidin-4-amine libraries under microwave irradiation (MWI) is reported. The one-pot microwave-assisted synthetic protocol is high-yielding, ecofriendly, rapid, and novel as well as eliminates intermittent workups. The protocol can be adapted for the library synthesis of series of a condensed pyrimidines.

GRAPHICAL ABSTRACT

Keywords:

• Condensed 2H-pyrimidin-4-amines
• MWI
• one-pot synthesis

ACKNOWLEDGMENTS

The authors acknowledge the contributions of M. N Navale, president, and S. M. Navale, secretary, Sinhgad Technical Education Society, Pune, for providing encouragement, facilities to carry out the synthetic work, and basic spectroscopic analysis. The spectral and elemental analyses were done at the Department of Chemistry, Saurashtra University, Rajkot, Gujarat, India, and the Department of Chemistry University of Pune, India, respectively.