Abstract

An efficient and greener synthesis of a series of dihydropyrimidinone (DHPMs) derivatives were accomplished via three-component one-pot cyclocondensation between substituted aryl aldehydes, diketone/ke- toester and urea. This solvent free approach is totally nonpolluting having several advantages such as shorter reaction time, mild reaction conditions, simple workup and reduced environmental impact.

Highlights

  • Among the challenges for chemists include discovery and development of non-hazardous and simple environmentally safe chemical processes for selective synthesis by identifying alternative reaction conditions and solvents for much improved selectivity, energy conservation and even less hazardous waste generation are not desirable and inherently safer chemical products

  • In continuation of our research work in application of natural acids as catalyst, here, we report a solvent free one pot cyclocondensation reaction of substituted aryl aldehydes, diketone/ketoester and urea (Scheme 1) with good yields

  • Much effort has been made recently to improve and modify this reaction. This gave inspiration to organic chemists to find out more suitable protocol and simpler methods for the synthesis of DHPM and its derivatives are found in a large family of natural products with broad biological activities, due to which they become important classes of organic compounds

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Summary

Introduction

Among the challenges for chemists include discovery and development of non-hazardous and simple environmentally safe chemical processes for selective synthesis by identifying alternative reaction conditions and solvents for much improved selectivity, energy conservation and even less hazardous waste generation are not desirable and inherently safer chemical products. We have used this extract as natural catalyst for synthesis of DHPMs. The Italian chemist Pietro Biginelli (1893, University of Florence) for the first time reported on the acid-catalyzed cyclocondensation reaction of ethyl acetoacetate, benzaldehyde, and urea [12]. Much effort has been made recently to improve and modify this reaction This gave inspiration to organic chemists to find out more suitable protocol and simpler methods for the synthesis of DHPMs. DHPM and its derivatives are found in a large family of natural products with broad biological activities, due to which they become important classes of organic compounds. DHPM and its derivatives are found in a large family of natural products with broad biological activities, due to which they become important classes of organic compounds They generally possess intriguing therapeutic and pharmacological properties [13,14,15].

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