K. Ngu et Dv. Patel, PREPARATION OF ACID-LABILE RESINS WITH HALIDE LINKERS AND THEIR UTILITY IN SOLID-PHASE ORGANIC-SYNTHESIS, Tetrahedron letters, 38(6), 1997, pp. 973-976
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-a
lkylations with structurally and electronically diverse sets of alipha
tic and aromatic amines. Amongst the various resins modified and evalu
ated in this study, Wang resin derived bromo resin (3, X = Br) offers
the best practical choice with respect to loading, stability and chemi
cal reactivity. (C) 1997, Elsevier Science Ltd.