反应详情

TBTU (1.1 g) and diisopropylethylamine (1.1 g) were added to a solution of 2-ethyl-2H-pyrazole-3,4-dicarboxylic acid 4-ethyl ester (610 mg) in DMF (7 ml), and the mixture was stirred for 30 min at RT. 2-Phenyl-imidazo[1,2-a]pyrimidin-7-ylamine (example 1, step 1, 725 mg) was added to the light yellow solution, and the mixture was stirred over the weekend at RT. Water (15 ml) was added, and the mixture was stirred for an additional 15 min. For purification, the precipitate was suspended in DMF (5 ml) and water (10 ml), and filtered; this process was repeated 4 times. The thus obtained title compound (150 mg, 13%) was dried under vacuum.

1. stirringthe mixture was stirred over the weekend at RT
2. stirringthe mixture was stirred for an additional 15 min
3. customFor purification
4. filtrationwater (10 ml), and filtered