Affiliation:
1. Drug Discovery Chemistry Idorsia Pharmaceuticals Ltd. CH-4123 Allschwil Switzerland
Abstract
AbstractChromanes 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.
Subject
Inorganic Chemistry,Organic Chemistry,Physical and Theoretical Chemistry,Drug Discovery,Biochemistry,Catalysis