Synthesis of a Bisubstrate‐Type Inhibitor of N‐Acetylglucosaminyltransferases

Transfer interference: Synthesis of the bisubstrate-type N-acetylglucosaminyltransferase (GnT) inhibitor 1 was achieved by a polymer-resin hybrid capture–release strategy for the construction of the acceptor component. One-pot ligation in aqueous media produced the coupling product, and subsequent construction of a diphosphate linkage led to 1. Inhibitory activities toward GnT-V and GnT-IX were evaluated and revealed the potency of 1 toward the latter enzyme.