RAPID DECONVOLUTION OF COMBINATORIAL LIBRARIES USING HPLC FRACTIONATION

The rapid deconvolution of combinatorial libraries prepared via soluti on-phase simultaneous addition of functionalities is demonstrated usin g HPLC. Libraries containing 25-216 members are screened for biologica l activity, and active libraries are fractionated into discreet pools using reversed-phase HPLC. The entire process can be completed from a single synthesis of 15-50 mg, without the need for fixed positions, se rial synthesis, or tagging. The method is demonstrated for libraries w ith charged and uncharged functional groups, and for a library contain ing substituted benzyl moieties. (C) 1998 Published by Elsevier Scienc e Ltd. All rights reserved.