| 摘要 |
The invention comprises 1-cycloalkylmethyl-5-phenyl-7-halo-1H-1,4-benzodiazepin-2(3H)-ones and the preparation thereof by reacting the corresponding N1 unsubstituted compound with a cycloalkylmethylating agent. The preferred compound is 1-cyclopropylmethyl-5-phenyl-7-chloro - 1H - 1,4 - benzodiazepin - 2(3H)-one, which is prepared using e.g. cyclopropylmethyl bromide, cyclopropylmethyl b -naphthalenesulphonate or cyclopropyl tosylate. The reaction is preferably carried out in the presence of a strong base, e.g. sodium hydride. Therapeutic compositions, which are useful as tranquilizers and which may be administered as tablets, capsules, elixirs or suspensions, or parenterally, comprise as active ingredient the 1 - cycloalkylmethy' - 5 - phenyl - 7 - halo - 1H - 1,4 - benzodiazepin - 2(3H) - ones described above.
|
