Late-Stage Functionalization

The term late-stage functionalization (LSF) is recent but is now frequently used in the field of organic methodology development to describe transformations on complex molecules. Such reactions include catalytic and non-catalytic reactions, C–H functionalizations, and functional-group manipulations with one or several desired products. However, explicit guidance to classify whether a reaction is a LSF or not, and why or why not, is not available. Herein, we advance a definition for LSF and highlight the requirements, features, and challenges of LSF reactions accompanied by representative examples. We aspire that our analysis will be helpful as a guiding principle in the field.