The Heck reaction for synthesis of novel kinase inhibitors.
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- Institutt for kjemi 
Reaction conditions were investigated and developed for coupling of acrylates withdifferent properties. A total of seven acrylic thienopyrimidines weresynthesized, five of which were synthesized directly with the Heck reaction. Testing of in vitro enzymatic inhibition activity indicated that the acrylic moietieshas potential as very selective inhibitors, but due cis-trans isomerization problems,they are unsuitable for pharmaceutical use. Computer calculations indicate thatthe bioavailability properties of the acrylic moiety are improved, compared to thearyl moiety. Several acrylates were tested as a result of the project and the thesispostulates some new and stable, potential candidates with similar biological interactions.