反应详情

The mixture of 6-[3-(ethoxycarbonyl)-2-(4-fluorobenzyl)-5-oxo-7,8,9,9a-tetrahydro-5H-pyrido[2,3-α]pyrrolizin-4-yl]-3-pyridazinecarboxylic acid (G, 33 mg, 0.07 mmol), furfurylamine (19.3 mmol, 0.14 mmol), 1-(3-Dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride (26.7 mg, 0.14 mmol) and 1-hydroxybenzotriazole hydrate (18.8 mg, 0.14 mmol) in 2 ml dichloromethane was stirred for 2 hours. The mixture was then partitioned between water and ethyl acetate. The organic was washed with brine and dried over sodium sulfate. The residue upon the removal of the solvent was purified with flash chromatography. Twelve (12) mg white solid was obtained. NMR (400 MHz, CDCl3) δ 8.38 (d, 1H), 8.08 (d, 1H), 7.20 (t, 2H), 6.92 (t, 2H), 4.78 (m, 1H), 4.67 (d, 2H), 4.40 (dd, 2H), 3.90 (q, 2H), 3.64 (m, 1H), 3.39 (m, 1H), 2.48 (m, 1H), 2.35 (m, 2H), 1.40 (m, 1H), 0.90 (t, 3H) ppm. ESI-MS m/z 556 (M+H)+.

1. customThe mixture was then partitioned between water and ethyl acetate
2. washThe organic was washed with brine
3. dry with materialdried over sodium sulfate
4. customThe residue upon the removal of the solvent
5. customwas purified with flash chromatography
6. customwas obtained