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ABSTRACT: The presented research demonstrated solvent free, microwave-assisted one-pot synthesis of derivatives of 1, 3-diazacyclopenta-2, 4-diene. The targeted moiety being a dynamic class of N-heterocycles had remained at the forefront of biological and medicinal chemistry throughout since they were important pharmacophores encompassing vast significant activities. Owing to the potency and wide applicability of this moiety, a diversity-oriented convergent synthesis through multicomponent cyclocondensation of dicarbonyl substrates with numerous aryl aldehydes and ammonium acetate was carried out by employing two active catalysts individually. In addition, the catalytic performance in the synthesis of the desired compounds was also successfully evaluated and the compounds were also tested again two bacterial strains. This protocol produced pure products in high yield within a short period having the enhancing features of easy work-up and a high degree of atom economy.
KEYWORDS: One-pot synthesis, microwave-assisted synthesis, 1, 3-diazacyclopenta-2, 4-diene, multi-component reaction, cyclocondensation.
(Received 14-10-2016 Accepted 10-03-2018)
INTRODUCTION
Microwave-assisted high-speed chemistry has much to propose to the synthestic chemist due to its multiple advantages. The influence of micro-waves on stereo selectivity, regioselectivity and chemoselectivity along with the enormous accelerations resulting in speedy molecular interactions causing higher yield and purity as well are attributes that cannot be overlooked without contemplation (Jayabharathe et al., 2015). A merit of such distinguished attributes has empowered this technique to successfully carry out all formerly conventional synthesis along with those reactions that are incompatible with conventional heating. Thus, microwave-assisted organic transformations are an influential mean of rapidly exploring "chemistry space" and constructing structurally diverse libraries of active compounds (Gupta and Paul, 2012).
In addition, green approach has revolutionized the synthetic chemistry by focusing on the intrinsic hazards of a chemical and attempting to eliminate the use and generation of such perilous substances. Based on a set of 12 principles, green chemistry targets from the environmental protection to the energy efficiency and atom economy of a protocol thus contributing to overcome the debt to mother nature in terms of pollution (Teimouri and Chermahini, 2011).
Owing to the emergence of previously unknown complicated diseases, deadly infections and a drugresistance to old plagues, a global public health dilemma has been created. In an effort to overcome it and formulate exotic potential medicinal molecules for the augmentation of new drugs, novel synthetic strategies...