Carbohydrate Scaffolds for Combinatorial Syntheses That Allow Selective Deprotection of All Four Positions Independent of the Sequence

摘要

Combinatorial chemistry has accelerated the syntheses of novel active compounds in both pharmaceutical and agrochemical industries. To carry out solution-phase parallel combinatorial syntheses, sophisticated robots have been developed, but the applied procedures are limited by the total number of synthetic operations achievable. Thus, combinatorial syntheses on solid support remain particularly important for the generation of libraries of active compounds with highly diverse structures. Besides linear sequential syntheses of peptides and peptidomimetic compounds as the origin of combinatorial chemistry, and multicomponent reactions, selective transformations on multifunctional scaffolds are increasingly attractive for combinatorial applications. In this sense cyclopeptides with various side chains, bile acid derivatives, aryl- and squaric acid building blocks have been combinatorially applied as scaffolds for the introduction of side chains.