The asymmetric synthesis of 3,4-dihydropyrimidin-2-(1H)-one thioacetals was achieved for the first time using a chiral imidodiphosphoric acid catalyst. The Biginelli reaction involving aromatic aldehydes, thiourea, and 1,3-cyclohexanedione as multi-component reaction was conducted in ethyl acetate at 40°C with chiral imidodiphosphoric acid catalyst. Under mild conditions, a series of chiral polycyclic 3,4-dihydropyrimidin-2-(1H)-one thioacetals were obtained with high yields and excellent enantioselectivity (up to 99% ee).

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