反应详情

温度

110 °C

4-Amino-2-methyl-10H-thieno-[2,3-b][1,5]benzodiazepine (5 g, 0.02 mol), N-methylpiperazine (12.5 mL, 2.5 vol) and 1-propanol (15 mL, 3 vol) were charged into a three-necked round bottom flask equipped with a reflux condenser, overhead stirrer, and thermometer. The reaction mixture was heated slowly to 110° C. under a nitrogen atmosphere and then refluxed overnight. The reaction mixture was cooled to below 50° C. whereupon water (15 mL, 3 volumes) was added to precipitate out the solid, which was isolated by Buchner filtration. The resulting light yellow solid was washed twice with water (5 mL) and dried to afford olanzapine in 89% yield (5.22 g).

1. customequipped with a reflux condenser, overhead stirrer
2. temperaturerefluxed overnight
3. additionwas added
4. customto precipitate out the solid
5. customwhich was isolated by Buchner filtration
6. washThe resulting light yellow solid was washed twice with water (5 mL)
7. customdried