A series of analogous arrays of small, non-peptidyl, non-oligomeric co
mpounds were synthesized on polystyrene resin. With the aid of a funct
ionally differentiated phenolic scaffold, the batch preparation of uni
que benzamide and urea resins was accomplished, which were further der
ivatized in modified 96-well plates. An efficient cleavage reaction of
the phenyl benzoate link enabled the isolation of more than 600 pheno
lic compounds in milligram quantities that were suitable for direct bi
ological screening. The technology described herein represents a facil
e, economical approach to non-peptidyl chemical diversity.