Dimethylformamide → Trifluoroacetate

Participants

Reaction Steps

To a suspension of 8-(5-amino-2-trifluoromethoxy-phenylamino)-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide (146 mg, 0.4 mmol) in anhydrous dimethylformamide (5 mL) TBTU (190 g, 0.6 mmol) HOBT (81 mg, 0.6 mmol), and DIPEA (0.104 ml, 0.6 mmol) were added. The mixture was stirred at room temperature for 30 minutes. Then BOC-L-proline (129 mg, 0.6 mmol) was added and the reaction was stirred for an additional 3 h. The reaction mixture was diluted with water and the precipitate was collected, diluted with DCM (10 mL) and treated with TFA (1 mL). Evaporation of the solvent gave the title compound as trifluoroacetate salt (113 mg, 44% yield).

Provenance & Evidence