4-Methylmorpholine → rac-Methyl 4,4,4-trifluoro-2-[({8-[(3-fluoropyridin-2-yl)methoxy]-2,6-dimethylimidazo[1,2-a]pyridin-3-yl}carbonyl)amino]butanoate

Participants

Reaction Steps

250 mg (0.71 mmol) of 8-[(3-fluoropyridin-2-yl)methoxy]-2,6-dimethylimidazo[1,2-a]pyridine-3-carboxylic acid hydrochloride from Example 121A were initially charged in 4.1 ml of DMF, and 274 mg (0.85 mmol) of TBTU and 0.47 ml (4.26 mmol) of 4-methylmorpholine were added. 221 mg (1.07 mmol) of methyl 2-amino-4,4,4-trifluorobutanoate hydrochloride from Example 75A were then added, and the reaction mixture was stirred at RT overnight. About 32 ml of water were added to the mixture. The precipitated solid was filtered off, washed with water and dried under high vacuum. This gave 298 mg (68% of theory, purity 76%) of the target compound.

Provenance & Evidence