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Abstract

An efficient and facile one pot synthesis of 3,4-dihydropyrimidinones (Belinelli compound) from furfural, acetylacetone and urea under solvent free conditions was performed, resulted in promising yield. These compounds reacted with benzaldehyde and furfural to give the corresponding chalcones. Chalcones are used to synthesize several derivatives like pyrazolines isoxazoles and pyrimidines having different heterocyclic ring systems.

Keywords: Belinelli compounds; Chalcone; Pyrazolines isoxazoles; Pyrimidines

Introduction

Biginelli In 1893, the synthesis of functionalized 3,4-dihydropyrimidin-2(1H)-ones (DHPMs) scheme I via three-component condensation reaction of an aromatic aldehyde, urea and acetyl acetone was reported for the ?rst time by P. Biginelli. Within the past decades, such Biginelli-type dihydropyridines have gotten a significant sum of consideration due to the curiously pharmacological properties related with this heterocyclic scaffold. one-pot amalgamation could be a methodology to make strides the effectiveness of a chemical response whereby a reactant is subjected to progressive chemical responses in fair one reactor. This is much desired by chemists because avoiding a lengthy separation process and purification of the intermediate chemical compounds would save time and resources while increasing chemical yield. Many dihydropyridines and their derivatives are pharmacologically [1,2] important as calcium channel blockers, antihypertensive agents, and biological activities [3] also contain the dihydropyrimidinone-5-carboxylate core. Therefore, many synthetic methods for preparing such compounds have been developed [4]. Chalcones, one of the major classes of characteristic items with far reaching event in natural products, vegetables, flavors and soy-based foodstuff, have been detailed to have a few organic exercises such as anti-inflammatory [5], antibacterial [6], anti-fungal [7], and anti-tumor [8], antioxidant [9] and antimalarial activities [10]. In expansion of being utilized in pharmaceutical businesses, chalcones moreover discover wide applications in colors [11]. Separated from being naturally imperative compounds, chalcone subsidiaries appear non-linear optical (NLO) properties with great blue light transmittance and great crystallizable [12]. A vital include of chalcones is their capacity to act as a halfway for the union of organically dynamic heterocyclic compounds such as, pyrimidine and cyclohexanone derivatives [13]. The chemistry of chalcones has created seriously logical ponders all through the world. Particularly intrigued has been centered on the blend and biodynamic exercises of chalcones. The title “Chalcones” was given by Kostecka and Tambor [14]. These compounds are moreover known as benzalacetophenone or benzylidene acetophenone. In chalcones, two fragrant rings are connected by an aliphatic three carbon chain. Chalcone bears a really great synthon so that assortment of novel heterocycles with great pharmaceutical profile can be outlined. Chalcones are unsaturated ketone containing the responsive ketoethylenic bunch –CO-CH=CH-. These are colored compounds since of the nearness of the chromophore -CO-CH=CH-, which depends within the nearness of other auxochromes. Different strategies are accessible for the planning of chalcones[15-17].The most helpful strategy is the Claisen-Schmidt condensation of equimolar amounts of arylmethyl ketone with aryl aldehyde within the nearness of alcoholic alkali[18].Chalcones are utilized to synthesize a few subordinates like cyanopyridines, pyrazolines isoxazoles and pyrimidines having distinctive heterocyclic ring frameworks [19-21].Besides, these are vital intermediates in numerous expansion responses of nucleophiles due to inductive polarization of carbonyl gather at the ?- position. These discoveries clarify the critical intrigued of researcher in this specific bunch of compounds. A few procedures for the union of these framework, based on the arrangement of carbon carbon bond have been detailed. Among them the coordinate Aldol condensation and Claisen-Schmidt condensation still possess unmistakable positions. The most strategy for the blend of chalcones is the classical Claisen-Schmidt condensation within the nearness of fluid antacid bases [22-27].

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References

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