反应详情

A stirred mixture of 8-chloro-1-(chloromethyl)-6-phenyl-4H-s-triazolo[4,3-a][1,4]benzodiazepine (1.37 g., 0.004 mole), potassium iodide (0.67 g., 0.004 mole), pyrrolidine (0.853 g., 0.012 mole) and tetrahydrofuran (100 ml.) is kept at ambient temperature (25° C.) for 18 hours and then concentrated in vacuo. The residue is mixed with water and extracted with methylene chloride. The extract is washed with brine, dried over anhydrous sodium sulfate and concentrated. The residue is crystallized to give 8-chloro-1-(pyrrolidinomethyl)-6-phenyl-4H-s-triazolo[4,3-a][1,4]benzodiazepine.

1. customis kept at ambient temperature
2. custom(25° C.)
3. customfor 18 hours
4. concentrationconcentrated in vacuo
5. additionThe residue is mixed with water
6. extractionextracted with methylene chloride
7. washThe extract is washed with brine
8. dry with materialdried over anhydrous sodium sulfate
9. concentrationconcentrated
10. customThe residue is crystallized