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. 2020 May 18;5(21):11923–11934. doi: 10.1021/acsomega.9b03910

Scheme 1. Synthetic Scheme Used for the Preparation of Fluoroquinolones including Novel N1-Benzofused Analogues.

Scheme 1

(i) (EtO)3CH, Ac2O, 140 °C, 3 h. (ii) R–NH2, DCM, rt, 15 h. (iii) DBU, LiCl, DCM, 45 °C—rt, 17.5 h. (iv) HCl, AcOH, reflux, 2.5 h. (v) Boc-piperazine, K2CO3, DMF, reflux, 15 h. (vi) TFA, dry DCM, rt, 2 h. (vii) 4 M HCl in dioxane, DCM, rt, 1 h. The seven fluoroquinolone compounds synthesized as a part of this study were three control compounds (ciprofloxacin, norfloxacin, and an N-benzyl analogue; 6a–c) and four novel N1-benzofused analogues (6d–g).