反应详情

A solution of 8-(2-chlorophenyl)-9-(4-chlorophenyl)-N-[(3R)-piperidin-3-yl]-9H-purin-6-amine (20 mg, 0.046 mmol, 1 eq.) in 1 mL of acetic anhydride and 1 mL of pyridine was stirred for 16 h. The reaction was concentrated in vacuo. The crude material was purified by silica gel column chromatography using 0-100% ethyl acetate/hexanes to yield 19 mg (87%) of 1-[(3R)-3-{[8-(2-chlorophenyl)-9-(4-chlorophenyl)-9H-purin-6-yl]amino}piperidin-1-yl]ethan-1-one. 1H NMR (300 MHz, CHLOROFORM-d) δ ppm 1.53-1.92 (m, 3 H) 2.07 (br. s., 4 H) 2.84-3.37 (m, 2H) 3.86-4.59 (m, 3 H) 5.88 (br. s., 1 H) 7.04-7.60 (m, 8 H) 8.37 (br. s., 1 H), [M+H]+ 481.3.

1. concentrationThe reaction was concentrated in vacuo
2. customThe crude material was purified by silica gel column chromatography