1,2-Difunctionalizations of alkynes entailing concomitant C–C and C–N bond-forming carboamination reactions

Vicinal carboamination of alkynes is a highly reliable and efficient practical strategy for the quick preparation of valuable and diverse amine derivatives starting from simple synthons. The last decade has witnessed numerous practical methods employing transition-metal-based/metal-free carboamination approaches using alkynes for the synthesis of these N-bearing entities. Driven by the renaissance of transition metal catalysis, intermolecular and intramolecular carboamination of alkynes comprising concomitant C–N and C–C bond formation has been studied extensively. In contrast to metal catalysis, though analogous metal-free approaches have been relatively less explored in the literature, they serve as alternatives to these expensive approaches. Despite this significant progress, reviews documenting such examples are sporadic; as a result, most reports of this type remained scattered throughout the literature, thereby hampering further developments in this escalating field. In this review, different conceptual approaches will be discussed and examples from the literature will be presented. Further, the reader will get insight into the mechanisms of different transformations.

The 1,2-difunctionalization of alkynes happening through concomitant C–C and C–N bond formation strategies have provide an unified access to diversely functionalized N-bearing heterocycles.