new derivatives of azepine and their preparation.

摘要

The invention comprises: (a) 3-alkanoyl-10,11-dihydro-5-dibenzo[b.f]azepines of the general formula FORM:0912013/IV (b)/1 wherein X represents -CH2-CH2-and R1 an alkyl radical of 1-3 carbon atoms; (b) the preparation of compounds I by reacting, in the presence of a Friedel-Crafts condensing agent, a 5-acyl-10,11-dihydro - 5 - dibenzo[b.f]azepine with a halide or anhydride of a C2-4 alkane-carboxylic acid and hydrolising the resulting 3-alkanoyl-5-acyl compound; (c) the combination of (b) with the Wolff-Kishner reduction of the product to a compound of the general formula FORM:0912013/IV (b)/2 (wherein X represents -CH2-CH2- and R2 an alkyl radical of 2-4 carbon atoms) by treatment with hydrazine and an alkali metal hydroxide or alcoholate; and (d) the combination of (c) with the conversion of the products to the corresponding compounds in which X represents -CH=CH- by acylation to form an easily split 5-acyl derivative, reaction of this with halogen or a compound giving off halogen, reaction of the resulting 3-alkyl-5-acyl-10-halo compound with an agent splitting off hydrogen halide, and simultaneous or subsequent hydrolysis to remove the 5-acyl substituent. Compounds II are useful as intermediates for the synthesis of pharmaceuticals.