Abstract

The one-pot three-component reaction of 2-aminobenzothiazole, benzaldehyde derivatives and β-ketoester, β-diketone or malonate derivatives in solvent-free conditions provides the corresponding pyrimido [2,1-b] benzothiazole derivatives at 60?C in 60% - 72% yields without using any catalyst in an optimistic time.

Highlights

  • Fused heterocyclic compounds are very important compounds partially because of their pharmacological properties which include wide applications in medicinal chemistry [1]

  • Much attention has been drawn to pyrimidines and condensed pyrimidine compounds for their worthwhile and interesting biological properties [2]

  • Pyrimido[2,1-b]benzothiazole derivatives are evaluated for their High affinity central benzodiazepine recep tor ligands [3,4]

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Summary

Introduction

Fused heterocyclic compounds are very important compounds partially because of their pharmacological properties which include wide applications in medicinal chemistry [1]. The pharmaceutical properties of these ligands range from anxiolytic/anticonvulsant for agonists to antigenic/convulsant for inverse agonists and it has been used for treating patients diagnosed with epilepsy These compounds are incorporated with pyrazole structure known to possess tranquilizing, psychoanalytic and muscle relaxant activities [5,6,7]. The above methods that have been described for the synthesis of pyrimido[2,1-b]benzothiazole derivatives have their own advantages, but many of these reported procedures lead to some disadvantages including low yields, prolonged reaction time, various use of reagents, catalysts, toxic organic solvents in the reaction media as well as high temperature during completion of the reaction. In continuation of our research programs to find novel one-pot multicomponent reactions [30,31,32,33,34,35] we wish to report the one-pot three component reaction of benzaldehyde derivatives, active methylene compounds and 2-amino benzothiazole in solvent-free conditions. (Scheme 1)

Results and Discussion
Conclusion
Instruments and Characterization
Selected Data for Compounds 6a-g
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