High-Throughput Salt Screening of Synthetic Intermediates: Effects of Solvents, Counterions, and Counterion Solubility

Using a statistical Z-score methodology, the yield
data from 65 high-throughput acid screens and 45 base screens on synthetic
intermediates were analyzed. The results show that salt screening
outcomes are largely determined by the choice of counterions and solvents.
We rank-ordered counterions, solvents, and counterion/solvent combinations
and provided recommendations on how to carry out more productive high-throughput
salt screening on synthetic intermediates.