反应详情

温度

70 °C

Under an argon atmosphere, a solution of 130 mg (0.38 mmol) of the compound from Example 222A in 1 ml DMF and 2 ml DME at 0° C. is treated with 505 μl of an LiHMDS solution (1 M in THF, 505 μmol). The cooling bath is removed and the mixture stirred for 15 mins at RT before addition of 113 mg (505 μmol) of tert.-butyl 4-bromobutanoate. The mixture is stirred overnight at 70° C. After cooling, 0.5 ml of 1 N hydrochloric acid are added. The reaction mixture is then directly separated by preparative HPLC (Method 20). 48 mg (30% of theory) of the title compound are obtained.

1. customThe cooling bath is removed
2. temperatureAfter cooling
3. customThe reaction mixture is then directly separated by preparative HPLC (Method 20)