Abstract
Aromatic substitution enables the synthesis of relevant and promising biological entities through the direct synthesis of a range of highly functionalized compounds. Thus, since its discovery and over more than one century, the Friedel–Crafts (F-C) alkylation has been used for carrying out such a transformation. Despite its aptitude and viability for aromatic substitutions, it is quite surprisingly that catalytic and asymmetric versions of F-C reactions have only been described in the mid-1980s. In this microreview, we are planning to underscore the main and recent developments in organocatalyzed F-C reactions which were published within the 2001–2009 timeframe.