Preparation of acid-labile resins with halide linkers and their utility in solid phase organic synthesis

Article abstract of DOI:10.1016/S0040-4039(96)02502-6

Mild and efficient preparation of acid-labile resins with displaceable halide linkers (3 and 4, X = Br and I) is described. These resins can be used in combinatorial organic synthesis of numerous drug-scaffold libraries. Their synthetic utility is exemplified by high yielding N-alkylations with structurally and electronically diverse sets of aliphatic and aromatic amines. Amongst the various resins modified and evaluated in this study, Wang resin derived bromo resin (3, X = Br) offers the best practical choice with respect to loading, stability, and chemical reactivity.