反应详情

To a solution of 1-(4-aminoquinazoline-7-ylmethyl)piperazine-2-one bishydrochloride (1.84 g, 5.73 mmol), EXAMPLE 72, in DMF (20 mL) is added 2-bromomethyl-6-chloro-benzo[b]thiophene, EXAMPLE 5, (1.5 g, 5.73 mmol) and K2CO3 (4.0 g, 28.7 mmol). The solution is stirred for 16 hours. After this time, the solution is diluted with water. The solution is acidified with trifluoroacetic acid. The product is purified by RP-HPLC eluting in a gradient of 10% CH3CN/H2O (0.1% TFA) to 50% CH3CN/H2O (0.1% TFA). The appropriate collected fractions are lyopholized to afford the title compound as a white solid. 1H NMR (d6-DMSO, 300 MHz) δ9.78 (bs, 3H), 8.82 (s, 1H), 8.34 (d, 1H), 8.07 (s, 1H), 7.81 (d, 1H), 7.63 (d, 1H), 7.51 (s, 1H), 7.32 (m, 2H), 4.71 (s, 2H), 3.95 (s, 2H), 3.28 (m, 4H), 2.80 (m, 2H).

1. customThe product is purified by RP-HPLC
2. washeluting in a gradient of 10% CH3CN/H2O (0.1% TFA) to 50% CH3CN/H2O (0.1% TFA)
3. customThe appropriate collected fractions