反应详情

温度

25 °C

To a stirred solution of methyl (1R,2S)-2-[(3-methylbenzyl)amino]cyclopentane-carboxylate (74 mg, 0.30 mmol) and (7-methanesulfonylamino-1,1-dioxo-1,4-dihydro-1λ6-benzo[1,2,4]thiadiazin-3-yl)-acetic acid (prepared as described in Example 1j, 100 mg, 0.30 mmol) in anhydrous N,N-dimethylformamide (3 mL) under a nitrogen atmosphere, N-methylmorpholine (0.10 mL, 0.9 mmol) and 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride (63 mg, 0.33 mmol) were added sequentially. The mixture was stirred at 25° C. for 16 h, diluted with ethyl acetate, washed with 1.0 M aqueous hydrochloric acid and saturated aqueous brine solution, dried over magnesium sulfate and filtered. The filtrate was concentrated in vacuo to afford the amide intermediate, which was used directly in the next step without further purification.

1. washwashed with 1.0 M aqueous hydrochloric acid and saturated aqueous brine solution
2. dry with materialdried over magnesium sulfate
3. filtrationfiltered
4. concentrationThe filtrate was concentrated in vacuo