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Keywords:

  • Paullone analogues;
  • Heck reaction;
  • Inhibitors;
  • Kinase inhibition

Abstract

The syntheses of paullone (1a) and three paullone derivatives, including a sulfur analogue (2a), a tricyclic derivative (2b), and a ring-enlarged variant (2c), are described, Pd-catalyzed intramolecular Heck reaction being the key step. The kinase-inhibitory properties of the novel paullone analogues were investigated.