Scalable Preparation of 1‐Aminoethyl Substituted Chromanes

Chromanes and chromanones are structural motives found in many bioactive compounds. To support structure‐activity‐relationship (SAR) studies in a medicinal chemistry program, we developed two alternative synthetic strategies to access 1‐aminoethyl chromane building blocks. Our strategies involve a C(sp2)−C(sp3) coupling for late‐stage introduction of the aminoethyl side chain. In addition, an optimized process was developed to enable decagram scale preparation of one building block.