PREPARATION OF ACID-LABILE RESINS WITH HALIDE LINKERS AND THEIR UTILITY IN SOLID-PHASE ORGANIC-SYNTHESIS

Authors
Citation
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
Citations number
10
Categorie Soggetti
Chemistry Inorganic & Nuclear
Journal title
ISSN journal
00404039
Volume
38
Issue
6
Year of publication
1997
Pages
973 - 976
Database
ISI
SICI code
0040-4039(1997)38:6<973:POARWH>2.0.ZU;2-G
Abstract
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.