反应详情

To a solution of (2S)-1-(2-methylbenzothiazol-5-yloxy)-3-piperazinylpropan-2-ol (800 mg, 2.6 mmol) in acetone (20 ml) was added propargyl bromide (80% solution, 0.290 ml, 2.6 mmol) and potassium carbonate (720 mg, 5.2 mmol). The solution was heated to reflux and stirred for 5 hours. Thin layer chromatography (10:1 dichloromethane:methanol) showed formation of product. The solution was cooled and filtered. The filtrate was concentrated and purified by preparative chromatography (dichloromethane:methanol) to yield (2S)-1-(2-methylbenzothiazol-5-yloxy)-3-(4-prop-2-ynylpiperazinyl)propan-2-ol (500 mg, M+1=346.2). B. Preparation of a Compound of Formula I

1. temperatureThe solution was heated
2. temperatureto reflux
3. temperatureThe solution was cooled
4. filtrationfiltered
5. concentrationThe filtrate was concentrated
6. custompurified by preparative chromatography (dichloromethane:methanol)