反应详情

2-Nitro-4-fluoro-5-(piperidin-1-yl)aniline (13.0 g, 52%) was prepared by an analogous procedure as described in preparation 1 (step 3) using N-(2-nitro-4-fluoro-5-chloro phenyl)acetamide (25.0 g, 0.107 mol) (obtained in preparation 1, step 2), piperidine (45.8 a, 0.537 mol), potassium hydroxide (9.0 g, 0.16 mol) and dimethyl sulfoxide (100 mL). mp 112-113° C. IR (KBr) 3472, 1234 cm-1 ; 1H NMR (CDCl3) δ 1.60 (m, 2H, CH2), 1.70 (m, 4H, (CH2)2), 3.22 (m, 4H, N(CH2)2), 5.88 (d, J=7.6 Hz, 1H), 6.08 (brs, 2H, NH2), 7.78 (d, J=14.2 Hz, 1H) ; Mass (m/z) 239 (M+.).

1. customas described in preparation 1 (step 3)