Ruthenium-catalysed direct C–H amidation of 4-aryl-pyrrolo[2,3-d]pyrimidines with acyl/phosphoryl azides

Abstract

A ruthenium-catalysed arene ortho C–H amidation of 4-aryl-pyrrolo[2,3-d]pyrimidine derivatives with acyl azides or phosphoryl azides as the nitrogen sources toward C–N bond formation was developed. This protocol could offer a novel and direct approach to access a series of amidated and phosphoramidated pyrrolo[2,3-d]pyrimidine derivatives in moderate to good yields, thereby evading the general Curtius rearrangement. The protocol features significant functional group tolerance and a single-step process, with the release of only innocuous molecular nitrogen as the byproduct.