An expedient synthesis of highly functionalized naphthyridones and quinolines from a common N-aryl pyridinone template

Org Lett. 2002 Jun 13;4(12):2071-4. doi: 10.1021/ol025950z.

Abstract

[reaction: see text] We describe herein a new base-mediated process for the formation of N-arylpyridinones 2 and their use for the preparation of naphthyridones and quinolines. The cyclization of various hindered enamines with methyl propiolate proceeds efficiently in the presence of NaOH to afford the corresponding N-arylpyridinones. These substrates were then found to undergo subsequent cyclizations to afford highly functionalized naphthyridones and quinolines.