反应详情

A mixture of 8.0 g of 11-(3-chloropropionyl)-5,11-dihydro-6H-pyrido-[2,3-b][1,4]-benzodiazepine-6-one and 30 ml of 1-benzyl-piperazine in 100 ml of isopropanol was refluxed for 1 hour. Then, the mixture was evaporated in vacuo to dryness and the residue was treated with sodium hydroxide solution. The base was extracted therefrom with chloroform and the chloroform extract was distilled to dryness. The residue was crystallized from xylene to obtain a 78% yield of 11-[3-(4-benzyl-1-piperazinyl)-propionyl]-5,11-dihydro-6H-pyrido-[2,3-b][1,4]-benzodiazepine-6-one with a melting point of 205°-207° C. The dihydro chloride salt of the acid base melted at 212°-214° C. after crystallization from methanol.

1. temperaturewas refluxed for 1 hour
2. customThen, the mixture was evaporated in vacuo to dryness
3. additionthe residue was treated with sodium hydroxide solution
4. extractionThe base was extracted
5. extractionwith chloroform and the chloroform extract
6. distillationwas distilled to dryness
7. customThe residue was crystallized from xylene