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The Heck reaction for synthesis of novel kinase inhibitors.

Willumsen, Fredrik Bysting
Master thesis
Åpne
10367_FULLTEXT.pdf (Låst)
10367_COVER.pdf (Låst)
Permanent lenke
http://hdl.handle.net/11250/2615613
Utgivelsesdato
2015
Metadata
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Samlinger
  • Institutt for kjemi [1017]
Sammendrag
Reaction conditions were investigated and developed for coupling of acrylates with

different properties. A total of seven acrylic thienopyrimidines were

synthesized, five of which were synthesized directly with the Heck reaction. Testing of in vitro enzymatic inhibition activity indicated that the acrylic moieties

has potential as very selective inhibitors, but due cis-trans isomerization problems,

they are unsuitable for pharmaceutical use. Computer calculations indicate that

the bioavailability properties of the acrylic moiety are improved, compared to the

aryl moiety. Several acrylates were tested as a result of the project and the thesis

postulates some new and stable, potential candidates with similar biological interactions.
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