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The efficient and novel approach for synthesizing cyanomethylated thiohydantoin from readily obtainable acetonitrile and 1,3-dibenzyl-2-thiohydantoin through iron(II)-catalyzed cross dehydrogenative coupling (CDC) protocol is documented here. The strategy displays extensive substrate scope, and provides an effectual construction of cyanomethylated thiohydantoins in moderate to good yield. Prominently, this new methodology represents hitherto unobserved reactivity pattern for the thiohydantoin.

The azepinone scaffolds are an important framework of pharmaceutically interesting compounds and many bioactive natural products. This review mainly focused on the metalcatalyzed approaches towards the synthesis of azepinones . Mainly it covers cycloisomerization and metal carbenoid insertion. It also involves transformations through cycloaddition reactions, metathesis reactions, microwave reactions and direct CÀ H/CÀ C/CÀ N activation reactions. The applications, substrate scope, limitations and plausible mechanisms of these transformations have also been discussed.