反应详情

Ethylamine (2 mL, 4.02 mmol, 2M soln in methanol) was added to a solution of 2-amino-5-methoxy-1,3-benzothiazole-7-carboxylic acid (300 mg, 1.34 mmol), diisopropyl ethylamine (0.93 mL, 5.36 mmol) and HATU (560 mg, 1.47 mmol) in DMF (6 mL). The reaction was stirred at ambient temperature for 2 hours after which time LCMS indicated clean conversion to the product. The reaction was diluted with EtOAc, washed with water and brine then dried (MgSO4), filtered and concentrated in vacuo. The crude material was purified by trituration with DCM to give the product as an off white solid, 178 mg, 53% yield.

1. washwashed with water and brine
2. dry with materialthen dried (MgSO4)
3. filtrationfiltered
4. concentrationconcentrated in vacuo
5. customThe crude material was purified by trituration with DCM
6. customto give the product as an off white solid, 178 mg, 53% yield