Solid phase synthesis of combinatorial libraries using anhydrides as templates

John Perumattam, Sarvajit Chakravarty, Glenn A. McEnroe, R. Richard Goehring, Babu Mavunkel, Sandhya Suravajjala, Whitney W. Smith, Baili Chen
Scios Inc., 820 West Maude Avenue, Sunnyvale, CA 94086, U.S.A.

Abstract
A simple and general approach to the synthesis of chemical libraries based on a universal anhydride template allows the preparation of large number of compounds. Various cyclic/acyclic amines, primary/secondary amines, differentially protected bifunctional amines were used as nucleophiles to react with anhydrides. The free carboxylic acid generated was then coupled with solid-bound amines. The facile and rapid generation of compounds through this multi-component assembly can be accomplished in a combinatorial parallel synthesis.

Keywords
anhydrides, assembly, chlorotrityl resin, combinatorial synthesis, diamines