A safety-catch linker for amine release under biologically compatible conditions
David Orain
Department of Chemistry, University of Southampton,
Southampton SO17 1BJ, U.K.
Mark Bradley
Department of Chemistry, University of Southampton,
Southampton SO17 1BJ, U.K.
(To whom correspondence should be addressed)
Abstract
A 'biocompatible' safety-catch linker based on an internal
diketopiperazine release has been developed to allow the release of amine
based compounds. The synthesis of the linker and its pre-loading with a
representative set of amines is described. After immobilization onto an
amino Tentagel resin, the linker was activated and the amines were
released under biological conditions at pH 8.
Keywords
amines, diketopiperazine, solid phase organic synthesis (SPOS)
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