A General Route to Cyclic Amidines and Isothioureas Based on Formal Aza Diels Alder Reactions of Aminoheterocycles
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文摘
2-Aminobenzothiazoles, 2-aminopyrazine, 1-aminoisoquinoline and 2-aminonaphthyridines all undergo reaction with formaldehyde and electron rich alkenes such as styrenes, cyclopentadiene, cyclohexadiene and indene to give cyclic amidines, or in the case of the benzothiazoles cyclic isothioureas. The relationship of the diverse series of skeletons, which are easily prepared, to compounds of known biological activity is emphasized.