反应详情

A solution of (5-cyclobutyl-thiazol-2-yl)-carbamic acid phenyl ester (Example 2; 35 mg, 0.128 mmol) and 6-amino-2-methyl-quinoline (50 mg, 0.128 mmol) in 1,4-dioxane (500 μl) were heated at about 70° C. for 24 hours. Purification by silica gel chromatography (1:3 hexanes-ethylacetate; 40:1→20:1 chloroform-methanol) and subsequent conversion to the HCl salt afforded 40 mg of the title compound. 1HNMR (400 MHz, CDCl3) δ 8.11(s,1H), 7.87 (s,7.88,1H), 7.85 (s,1H), 7.45 (d, J=7.6 Hz,1H), 7.16 (d, J=8.4 Hz, 1H), 6.94 (s,1H), 3.55 (m,1 H), 2.67 (s,3H), 2.35 (m,2H), 2.15-1.80 (m,4H). LRMS m/z (APCl+) 339.0 (M+H)+.

1. customPurification by silica gel chromatography (1:3 hexanes-ethylacetate; 40:1→20:1 chloroform-methanol) and subsequent conversion to the HCl salt