Fluoronaphthyridines and quinolones as antibacterial agents. 1. Synthesis and structure-activity relationship of new 1-substituted derivatives

D Bouzard, P Di Cesare, M Essiz…

Index: Bouzard, D.; Cesare, P. Di; Essiz, M.; Jacquet, J. P.; Remuzon, P.; et al. Journal of Medicinal Chemistry, 1989 ,  vol. 32,  # 3  p. 537 - 542

Full Text: HTML

Citation Number: 64

Abstract

33 35'(a) R'NH2, EtOH, room temperature;(b) NaH in dioxane or K2 C03 in acetone, or NBulF in THF;(c) NaOH, H20;(d) piperazine, fluoroaroyl)-3-ethoxyacrylate 29 with a slight excess of an appropriate amine in ethanol at room temperature gives the corresponding enamino keto ester 30, usually as a crystalline product. Cyclization of 30 (X= CH), by heating with sodium hydride in dioxane, gives ethyl 1, 4-dihydro-4-oxoquinoline-3-carboxylate. ...