Fluorinating Cleavage of Solid Phase Linkers for Combinatorial Synthesis

摘要

Organofluorine compounds play an increasingly important role in the modern drug discovery process. While the first fluorine-containing agent was developed in the late 1950s, today fluorinated pharmaceuticals and agrochemicals make up about 20% and 30% of their respective global markets. In 2006 two fluorinated drugs, the cholesterol-reducer Lipitor (1) and the asthma agent Advair, were the top-selling prescription drugs. Another fluorine-containing blockbuster drug of the last years is the antidepressant Prozac (2).