反应详情

Dichloromethane (0.75 mL) and DMA (0.75 mL) were added to N,N-diethylene-1,2-diamine (6 mg, 0.05 mmol). While the mixture was stirred, cis(±)-2-(4-{[(4-chloro-5-ethyl-1H-imidazol-2-yl)carbonyl]amino}-3-methoxypiperidin-1-yl)-4-methyl-1,3-thiazole-5-carboxylic acid obtained in Example (14a) (20 mg, 0.05 mmol), WSC hydrochloride (30 mg, 0.15 mmol) and HOBT (10 mg, 0.08 mmol) were added, followed by stirring at room temperature for one day. The reaction solution was diluted with ethyl acetate and aqueous sodium bicarbonate solution. The organic layer was washed with brine, dried over anhydrous magnesium sulfate, and then concentrated under reduced pressure. The residue was solidified with diethyl ether and hexane to obtain 11 mg of the title compound as a white solid (44%).

1. stirringby stirring at room temperature for one day
2. washThe organic layer was washed with brine
3. dry with materialdried over anhydrous magnesium sulfate
4. concentrationconcentrated under reduced pressure