反应详情

A 0.6 mL 5N HCl solution is added to a stirred solution of 1-chloro-isoquinoline-5-sulfonic acid {2-[2-(2-trifluoromethyl-phenoxy)-ethylamino]-ethyl}-amide (70 mg, 0.15 mmol) in THF (1 mL) at ambient temperature under nitrogen. The resultant mixture is heated at 65° C. for 16 hours. At ambient temperature, the mixture is concentrated. The crude product is dissolved in a small amount of MeOH/CH2Cl2 before it is treated with Et2O to form a white suspension. After filtration and vacuum drying, 24 mg (0.49 mmol, 33% yield) of the title compound is obtained as a white powder. ESIMS: m/z 456 (M+H)+.

1. concentrationAt ambient temperature, the mixture is concentrated
2. dissolutionThe crude product is dissolved in a small amount of MeOH/CH2Cl2 before it
3. additionis treated with Et2O
4. customto form a white suspension
5. filtrationAfter filtration and vacuum
6. customdrying