| 摘要 |
<p>Prepn. of 1,3-dihydro-7-nitro-5-phenyl-2H-1,4-benzodiazepin-2-one (I) of the formula: by treating 2-glycylamino-5-nitro-benzophenone (II) with agents which release protons (pref. weak or strong organic or inorganic acids such as HCOOH, AcOH, H3PO4, hydrohalic acids and H2SO4). Anticonvulsant, muscle-relaxant, hypnotic. Very good yields (>=80%), high purity. (II) may be readily obtd. in very good yields and in high purity, e.g. from 2-(O-arylsulphonyl-glycoloylamino)-5-nitrobenzophenones (III) and NH3. (II) need not be isolated before cyclisation to (I) (e.g. (III) can be reacted with NH3 in dioxan as solvent, then excess NH3 flushed from the reaction mixture with air and the reaction mixture acidified to cause cyclisation to (I)).</p> |
