反应详情

3-[4-(5-Bromo-thiophen-2-ylamino]-benzoic acid (20 mg, 0.048 mmol), prepared using method 2 (step 3) and 3-aminobenzoate, was combined with N-methylpiperazine (8.1 uL, 0.073 mmol), DIEA (29.2 uL, 0.168 mmol) and HATU (27.7 mg, 0.073 mmol) in a Smith microwave vial (0.2-5.0 mL) in 0.5 mL DMA. The mixture was micro waved at 90° C. for 900 s. The solution was diluted with 0.5 mL DMSO and purified by preparative HPLC to afford {3-[4-(5-Bromo-thiophen-2yl)-pyrimidin-2-ylamino}-phenyl}-(4-methyl-piperazin-1-yl)methanone (17.8 mg, 79.1%) after lyophilization. MS: m/z 458 (M+H+).

1. custompurified by preparative HPLC