Benzylation of 1,3-diketons in the phase transfer catalysis condition by microwave irradiation

Abstract

1,3-diketones as ethyl acetoacetate (EAA) and diethyl malonate (DEM) are widely used to obtain a wide range of highly effective excipients in fine organic synthesis, specially for pharmaceutical industry. Microwave (MW) radiation exposure can significantly speed up reactions and increase the exit of the targeted materials, reducing the resorption in organic synthesis. MW radiation is a crucial tool for the development of green chemistry. Advantages of this method are lack of heat, cleanliness of the reaction, practical instantaneous heating of the reaction mass to the given temperature and, in particular, replacing the traditional solvent with an elevated and polar solvent.1,2 In this presentation have comprised the studied technique of alkylation in the usual phase transfer catalysis (PTC) in the same PTC condition with the combination of MW technique for the choice more convenient conditions for this important product synthesis. It is had been known, that the combination of the MW–PTC techniques was used in the alkylation of active methylene containing substrates such as ethyl acetoacetate.3