反应详情

温度

25 °C

3-(RS)-Chloro-1,3-dihydro-5-(2-fluorophenyl)-2H-1,4-benzodiazepin-2-one (150 mg, 0.520 mmol) and 2-aminomethylindole (75.9 mg, 0.520 mmol) were combined in 1,2-dimethoxyethane (3 ml) and the mixture stirred 20 min. at 25° C. The mixture was evaporated to dryness in vacuo and the residue treated with H2O and extracted with EtOAc (3×). The combined extracts were washed with H2O (1×), dried over MgSO4, filtered and stripped to dryness in vacuo to give an orange oil which, after chromatography on silica gel (4% MeOH in CH2Cl2) provided the title compound as a white solid from ether: (m.p. 200°-202°).

1. customThe mixture was evaporated to dryness in vacuo
2. additionthe residue treated with H2O
3. extractionextracted with EtOAc (3×)
4. washThe combined extracts were washed with H2O (1×)
5. dry with materialdried over MgSO4
6. filtrationfiltered
7. customto give an orange oil which