反应详情

43 mg (0.4 mmol) of 3-methylazetidine hydrochloride, 100 mg (0.3 mmol) of the compound from Example 12A and 174 μl (130 mg, 1.0 mmol) of N-ethyl-N-(propan-2-yl)propane-2-amine are suspended in 2 ml of tetrahydrofuran and reacted in a single mode microwave (Emrys Optimizer) at 120° C. for 1.5 h. The reaction mixture is concentrated under reduced pressure, taken up in water with addition of aqueous 1 N sodium hydroxide solution (pH=9-10) and purified by preparative HPLC (RP18 column; mobile phase: acetonitrile/water gradient). Yield: 25 mg (25% of theory)

1. customreacted in a single mode microwave (Emrys Optimizer) at 120° C. for 1.5 h
2. concentrationThe reaction mixture is concentrated under reduced pressure
3. additiontaken up in water with addition of aqueous 1 N sodium hydroxide solution (pH=9-10)
4. custompurified by preparative HPLC (RP18 column; mobile phase: acetonitrile/water gradient)