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

โœ Scribed by Khehyong Ngu; Dinesh V. Patel

Publisher
Elsevier Science
Year
1997
Tongue
French
Weight
249 KB
Volume
38
Category
Article
ISSN
0040-4039

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โœฆ Synopsis

Mild and efficient preparation of acid-labile resins with displaceable halide linkers (3 and 4, X = Br and 1) 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.

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