Metal‐free catalysis: A method for the transamidation of primary amides with primary or secondary amines provides access to secondary and tertiary amides, by utilizing catalytic quantities of hydroxylamine hydrochloride to activate the chemically robust primary amide group (see scheme). A mechanism of primary amide activation through a hydrogen‐bonding complex is proposed.

Optimization of fragment hit 3 identified isoquinoline 45 as a potent inhibitor of NOTUM with an unexpected flipped binding mode.

No abstract