反应详情

(2-Chloro-[1,2,4]triazolo[1,5-a]pyridin-8-yl)-(2-methoxy-benzyl)-amine was prepared from 8-bromo-2-chloro-[1,2,4]triazolo[1,5-a]pyridine (2.00 g, 8.60 mmol) and 2-methoxy-benzylamine in a manner analogous to Example 2d. Product isolated as a tan oil that solidified upon standing (1.56 g. 63%). 1H NMR (400 MHz, (D3C)2SO, δ, ppm): 8.09 (d, J=6.7 Hz, 1H), 7.21 (m, 2H), 7.04-6.93 (m, 3H), 6.86 (t, J=14.5, 7.2 Hz, 1H), 6.35 (d, J=7.9 Hz, 1H), 4.43 (d, J=6.30 Hz, 2H), 3.86 (s, 3H). 387b) N(8)-(2-Methoxy-benzyl)-N(2)-[4-(4-methyl-piperazin-1-yl)-phenyl]-[1,2,4]triazolo[1,5-a]pyridine-2,8-diamine was prepared from (2-chloro-[1,2,4]triazolo[1,5-a]pyridin-8-yl)-(2-methoxy-benzyl)-amine (100.00 mg, 0.34634 mmol) and 4-(4-methyl-piperazin-1-yl)-phenylamine (74.2 mg, 0.388 mmol) in a manner analogous to Example 2d. Product isolated as a brown foam (23.79 mg, 15.5%). 1H NMR (400 MHz, (D3C)2SO, δ, ppm): 9.07 (s, 1H), 7.93 (d, J=6.2 Hz, 1H), 7.55 (d, J=8.4 Hz, 2H), 7.24 (m, 2H), 7.02 (d, J=8.4 Hz, 1H), 6.88 (m, 3H), 6.70 (t, J=13.70, 6.9 Hz, 1H), 6.29 (d, J=7.9 Hz, 1H), 6.09 (m, 1H), 4.46 (d, J=6.0 Hz, 2H), 3.87 (s, 3H), 3.02 (s, 4H), 2.45 (s, 4H), 2.22 (s, 3H). MS=444 (MH)+.

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