反应详情

To N-[4′-methyl-2-(morpholin-4-ylcarbonyl)-4,5′-bi-1,3-thiazol-2′-yl]-1H-imidazole-1-carboxamide, prepared as in Step 3 of Example 36, described above (75 mg; 0.19 mmol; 1 eq.), is added DMF (3 ml), Beta-alanine (Aldrich) (18.2 mg; 0.20 mmol; 1.10 eq.) and triethylamine (57 μl; 0.41 mmol; 2.20 eq.). The mixture is stirred 3 days at rt. Solvents are evaporated and the crude product is crystallized in MeOH, affording Compound (47) as a light yellow solid (17 mg; 22%). 1H NMR (DMSO-d6, 300 MHz) δ 2.41 (s, 3H), 2.49 (m, 4H), 3.31 (m, 6H), 4.33 (m, 2H), 6.71 (br s, 1H), 7.90 (s, 1H), 10.47 (br s, 1H), 12.34 (br s, 1H). M− (ESI): 424.03; M+ (ESI): 426.08. HPLC (method A), Rt: 2.20 min (purity: 98%).

1. customSolvents are evaporated
2. customthe crude product is crystallized in MeOH