Selective quantitative N-functionalization of unprotected α-amino acids using NHC-Ir(III) catalyst

Unnatural amino acids are valuable building blocks with numerous applications. Here, we present a quantitative technique for accessing mono-N-functionalized amino acids directly from unprotected substrates using alcohols as alkylating agents and an NHC-Ir(III) catalyst. We detail specific steps for catalyst preparation and application, as well as for catalyst recycling. The protocol excludes a few amino acids (l-cysteine, l-lysine, and l-arginine) and secondary alcohols. For complete details on the use and execution of this protocol, please refer to Bermejo-López et al. (2022).1.