Synthesis of fluorinated coumarines via isocyanide-based multi component reactions

The 3,4-dihydrocoumarin system is widely distributed in nature [1], and some derivatives have shown a wide range of biological activitiessuch as aldose reductase inhibition, antiherpetic, protein kinases, and a moderate estrogenic activity [2]. A variety of3,4- dihydrocoumarines were synthesized multi component reactions [3]. As a part of our current studies on the isocyanide-based multi component reactions, in this work,fluorinatedcoumarineshas been synthesized viafour-component reaction. A wide variety of pharmacologically significantand structurally interesting compounds were preparedviausing commerciallyavailablesubstituted 2-hydroxybenzaldehydes 1, Meldrum‘s acid 2, isocyanides 3,andfluoroalcohol4 inCH2Cl2 at room temperature without using any catalysts and activation in excellent overall yields (Scheme 1).Substituents could be independently varied at three different positions.