Resin-capture and release strategy toward combinatorial libraries of 2,6,9-substituted purines

J Comb Chem. 2002 Mar-Apr;4(2):183-6. doi: 10.1021/cc010080i.

Abstract

A resin-capture and release strategy for making combinatorial 2,6,9-trisubstituted purine libraries is demonstrated by capturing N9-derivatized purines at the C6 position with a thio-modified polymer. The C2 fluoro group is subsequently substituted with primary and secondary amines followed by thioether oxidation and release by C6 substitution with amines and anilines. This approach complements a previously reported strategy where a 6-phenylsulfenylpurine scaffold was captured at the C2 position with a resin-bound amine.(3)

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Combinatorial Chemistry Techniques
  • Enzyme Inhibitors / chemical synthesis*
  • Purines / chemical synthesis*

Substances

  • Enzyme Inhibitors
  • Purines