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Paper | Regular issue | Vol 57, No. 5, 2002, pp.857-870
Published online, 1st January, 1970
DOI: 10.3987/COM-02-9447
Synthesis of Heterocycle Substituted 1-Aryl-4-piperidones

Baihua Hu,* Michael Malamas, and John Ellingboe

*Chemical Sciences, Wyeth Research, Collegeville, PA 19426, U.S.A.


A series of heterocycle substituted 1-aryl-4-pipeidones were preparedvia Knoevenagel condensations between nitrogen-containing 5-membered heterocycles and benzaldehyde (1) followed by reduction or amination. Theoxadiazolidinedione ring was formed by reacting the N-hydroxyurea (10) with methyl chloroformate and sodium hydride.