反应详情

To a solution of 1,2,3,4-tetrahydro-isoquinoline-7-sulfonic acid dimethylamide (prepared according to the method of Example 247, Step B, 210 mg, 0.88 mmol) in isopropanol (5 mL) was added (R)-1-(4-chloro-pyrimidin-2-yl)-ethyl acetate (prepared according to the method of Preparation Five, 175 mg, 0.88 mmol) followed by triethylamine (0.24 mL, 1.75 mmol). This mixture was stirred at room temperature for 1.75 h then heated to reflux for 1.5 h, cooled to room temperature, evaporated, and purified by flash column chromatography (1% methanol/chloroform) to give 327 mg (92%) of the title compound of Example 247, Step C as a white solid.

1. customprepared
2. customaccording to the method of Preparation Five, 175 mg, 0.88 mmol)
3. temperaturethen heated
4. temperatureto reflux for 1.5 h
5. temperaturecooled to room temperature
6. customevaporated
7. custompurified by flash column chromatography (1% methanol/chloroform)