RECEPTOR SPECIFIC BINDER DISCOVERY USING INTRAMOLECULAR ACYL MIGRATION INDUCED DYNAMIC CARBOHYDRATE LIBRARY

摘要

An efficient molecular evolution system was obtained by combining two novel approaches in the field, intramolecular acyl migration for DCL generation and boronic acid as a selector. 1,4-Di-O-benzoyl chiro-inositol in acetonitrile with DBU as a base generated a reversible equilibrium of 9 regioisomers. Only 3,4-di-O-benzoyl chiro-inositol, containing two sets of cis-diols, is most favored toward binding with phenyl boronic acid, and its percentage of the DCL composition was amplified by up to 82%.