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Access to Paullone Analogues by Intramolecular Heck Reaction
Authors:Lionel Joucla  Florence Popowycz  Olivier Lozach  Laurent Meijer  Benoît Joseph
Affiliation:1. Laboratoire de Chimie Organique 1, UMR – CNRS 5181, Université Claude Bernard – Lyon 1, CPE – Batiment 308, 43 Boulevard du 11 Novembre 1918, F‐69622 Villeurbanne Cedex;2. Station Biologique – CNRS, Place G. Teissier, BP 74, F‐29682 Roscoff Cedex
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.
Keywords:Paullone analogues  Heck reaction  Inhibitors  Kinase inhibition
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