反应详情

温度

120 °C

A mixture of 1-benzenesulfonyl-4-chloro-5-nitro-1H-pyrrolo[2,3-b]pyridine (260 mg, 0.77 mmol), (R)-1-benzyl-3-aminopiperidine (175 mg, 0.92 mmol), diisopropylethylamine (197 μl, 1.16 mmol) in propan-2-ol (5 ml) was heated in a microwave reactor at 120° C. for 10 minutes. The mixture was diluted with DCM and then purified by column chromatography on silica gel (gradient: 0 to 40% ethyl acetate in cyclohexane) affording 429 mg of (1-benzenesulfonyl-5-nitro-1H-pyrrolo[2,3-b]pyridin-4-yl)-((R)-1-benzyl-piperidin-3-yl)amine, which was used for the next step without further purification. LCMS (Method B, ESI): RT=3.58 min, m+H=492.5; 1H NMR (400 MHz, CDCl3) δ: 9.53 (br s, 1H), 9.10 (s, 1H), 8.19-8.15 (m, 2H), 7.69-7.33 (m, 9H), 6.68-6.61 (m, 1H), 4.24-4.15 (br m, 1H), 3.54 (s, 2H), 2.77-2.27 (br m, 4H), 1.88-1.74 (br m, 3H), 1.69-1.52 (br m, 1H).

1. custompurified by column chromatography on silica gel (gradient: 0 to 40% ethyl acetate in cyclohexane)