反应详情

7-Morpholinopyrazolo[1,5-a]pyrimidin-5-amine (9A, 0.10 mmol) in pyridine (0.4 ml), cyclopropanecarboxylic acid (0.15 mmol) in pyridine (0.4 ml), HATU (0.17 mmol) in pyridine (0.4 ml) and DIEA (0.34 mmol) are mixed together before microwave irradiation at 150° C. for 6 minutes. The crude product was then purified by preparatory HPLC to give the titled compound. 1H NMR (400 MHz, CHLOROFORM-d) δ ppm 1.00-1.09 (m, 2 H) 1.09-1.16 (m, 2 H) 1.99-2.09 (m, 1 H) 3.91-3.98 (m, 4 H) 4.12-4.21 (m, 4 H) 6.47 (d, J=2.26 Hz, 1 H) 7.27 (s, 1 H) 7.51 (s, 1 H) 7.98 (d, J=2.07 Hz, 1 H) 13.03 (br. s., 1 H); ESI-MS: m/z 288 (M+H)+.

1. customThe crude product was then purified by preparatory HPLC