Synthesis of isoindolinones: Intramolecular [4+2] cycloaddition/retro [4+2] of pyridone propiolamides |
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Authors: | Jonathan E. Wilson Joshua Garvey Kennedy M. Taveras |
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Affiliation: | Constellation Pharmaceuticals, 215 First Street, Suite 200, Cambridge, MA 02142, United States |
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Abstract: | A new synthesis of isoindolinones was discovered during a screening campaign aimed at the development of novel methods for the synthesis of pyridone-EZH2 inhibitor analogues. The reaction proceeds via an intramolecular [4+2] cycloaddition of a pyridone with a tethered propiolamide moiety followed by extrusion of isocyanic acid. The discovery, optimization, and scope of the methodology are described. |
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Keywords: | Corresponding author. Isoindolinone Pyridone Cycloaddition Extrusion |
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