Discovery of Imidazo[1,2-]pyrazine Derivatives as Potent ENPP1 Inhibitors.

ENPP1 acts as a negative regulator of the cGAS-STING pathway through the hydrolysis of 2'3'-cGAMP. Inhibitors of ENPP1 are regarded as promising agents for stimulating the immune response in cancer immunotherapy. This study describes the identification and optimization of imidazo[1,2-]pyrazine derivative as a highly potent and selective ENPP1 inhibitor.

Rhodium(iii)-catalyzed switchable C-H acylmethylation and annulation of 2,2'-bipyridine derivatives with sulfoxonium ylides.

A novel protocol for Rh(iii)-catalyzed switchable C-H acylmethylation and annulation of 2,2'-bipyridine derivatives with sulfoxonium ylides is reported. This protocol provides a facile approach to synthesize structurally diverse acylmethylated 2,2'-bipyridine derivatives and acyl pyrido[2,3-a]indolizines with a broad range of functional group tolerance.