反应详情

The title compound was prepared according to the general procedure (Method B) by coupling Intermediate 13 (100 mg, 0.240 mmol) with 4-cyclopropyl-1,3-thiazol-2-amine (37 mg, 0.264 mmol) in the presence of EDCI hydrochloride (91 mg, 0.480 mmol) and DMAP (27 mg, 0.240 mmol) in a mixture of THF and DMF (1:1, 4 mL) to give 35 mg of the product as an off-white solid; 1H NMR (300 MHz, CDCl3) δ 0.79-0.85 (m, 2H), 1.05 (s, 9H), 1.20-1.26 (m, 2H), 1.95-2.01 (m, 1H), 3.58 (d, J=5.4 Hz, 2H), 6.60-6.71 (m, 1H), 6.90-6.98 (m, 1H), 7.10-7.27 (m, 3H), 7.38-7.46 (m, 1H), 7.50-7.56 (m, 2H), 7.63-7.70 (m, 1H), 7.92 (d, J=15.6 Hz, 1H), 7.99 (d, J=15.0 Hz, 1H), 13.03 (br s, 1H); APCI-MS (m/z) 539.45 (MH)+.