| 摘要 |
<p>Imidazo benzoxazepines of formula (I) and their salts are new. (where X = H, F, Cl, Br, NO2, 1-4C alkyl or alkoxy or CF3; R1 = H or 1-4C alkyl; R2 = H, SH, alkylthio, alkylsulphinyl or alkylsulphonyl of 1-6C, hydroxyalkylthio, hydroxyalkylsulphonyl, or hydroxysulphonyl of 1-4C or a group 1-4C alkyl or -(CH2)n-NR4R5; R4 & R5 are H, 1-4C alkyl, or together with the N atom = a 5 or 6 membered saturated heterocycle which may contain another O or N atom; m = 0, 1 or 2; n = 2 or 3). Used as CNS depressants and anticonvulsants. A typical cpd. is 4H, 10H imidazo 5,1-c (1,4)-benzoxazepine. This was prepd. by reducing a soln. of 3.3 g 1-(flurobenzyl)-5-hydroxymethyl imidazole in DMF with 1.2 g of a 55% dispersion of NaOH. The solvent was eliminated and the residue hydrolysed with water under N2. The yield was 1.4 g m.p.t. 139-142 degrees C.</p> |
