Solid/solution-phase annulation reagents: Single-step synthesis of cyclic amine derivatives

Spanning the diversity gap: The conversion of primary amines into cyclic derivatives is achieved by using a family of amine-derivatizing reagents, termed SPAn reagents (see scheme). The reagents, which require no further chemical manipulation or activation, are used to prepare discrete compounds or a library collection of diverse heterocycles. SPAn reagents have application in finding new lead compounds and the development of structure-activity relationships. (Equation Presented).