A new and improved process for celiprolol hydrochloride

…, MK Gurjar, NK Tripathy, MS Chorghade

Index: Joshi, Ramesh A.; Gurjar, Mukund K.; Tripathy, Narendra K.; Chorghade, Mukund S. Organic Process Research and Development, 2001 , vol. 5, # 2 p. 176 - 178

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Citation Number: 14

Abstract

The key intermediate in the synthetic sequence was 2-acetyl-4-nitrophenol (10). The literature offers two methods for its preparation: (a) the Fries migration 6 of 4-nitrophenyl acetate (9) and (b) nitration of o-hydroxy acetophenone. 7 The Fries migration of 4-nitrophenyl acetate (9) using 2.2 equiv of anhydrous AlCl 3 in dry nitrobenzene gave a 25% yield of 10 after steam distillation to remove nitrobenzene. Attempts to carry out the migration by heating a concentrated ...