摘要

Primary pyridylcarboxamides are prevalent parent structures in bioactive molecules and have the apparent advantages over N-protected derivatives as synthetic building blocks. However, no practical methods have been developed for direct synthesis of this compound class from unfunctionalized pyridines. We herein present a general, safe, concise, acid-free, and highly selective method for the C2-carbamoylation of pyridines with unprotected formamide and N-methyl formamide through the cleavage of two C-H bonds.