11-piperazinyldibenzo b f 1 4 oxazepins and thiazepins

摘要

Compounds of formula (I) R1 = H, alkyl, hydroxyalkyl; X = O or S. Also their acid addition salts. Tranquillisers and antidepressants. A mixture of 4-methyl-2'-(p-trifluoromethoxyphenyl)-1-piperazinecarboxanilide (2.5g), P2O5 (2.5g) and POCl3 (25 ml) was refluxed for 24 hr., the solution was evap. and the residue was treated with water. 6N HCl was added, the mixture was filtered and the filtrate was neutralised with NaOH and then basified with NaHCO3. The solution was extracted with ether and the dried extract was evap. The residue was dissolved in CH2Cl2 and chromatographed on a magnesia/silica gel column, eluting first with CH2Cl2 and then with a mixture of acetone/CH2Cl2. The solvent was evap. from the eluate to give 11-(4-methylpiperazino)-2-trifluoromethoxy-dibenzo (b,f) (1,4)-oxazepin which was converted to the hydrochloride with ethereal HCl. This compound provoked ataxia at 4mg/kg and depressed motor activity at 1.4mg/kg.