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 (3x). The combined extracts were washed with H2O (1X), 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 (3x)
4. washThe combined extracts were washed with H2O (1X)
5. dry with materialdried over MgSO4
6. filtrationfiltered
7. customto give an orange oil which