反应详情

温度

102 °C

4-Amino-2-methyl-10H-thieno-[2,3-b][1,5]benzodiazepine (100 g, 0.38 mol), N-methylpiperazine (250 mL, 2.5 vol) and 2-propanol (200 mL, 2 vol) were charged into a three-necked round bottom flask equipped with reflux condenser, overhead stirrer, and thermometer. The reaction mixture was heated to reflux at 102° C. under a nitrogen atmosphere overnight. The reaction mixture was allowed to cool to below 55° C. whereupon water (250 mL, 2.5 volumes) was added to precipitate out the solid. The light yellow solid was isolated by Buchner filtration and twice washed with 25% aqueous 2-propanol (100 mL) and then once with 2-propanol (100 mL). It was dried in vacuo to provide olanzapine in 86.5% yield (101.7 g).

1. customequipped
2. temperaturewith reflux condenser
3. temperatureThe reaction mixture was heated
4. additionwas added
5. customto precipitate out the solid
6. customThe light yellow solid was isolated by Buchner filtration
7. washtwice washed with 25% aqueous 2-propanol (100 mL)
8. customIt was dried in vacuo