首页> 外国专利> 11-AMINOALKYLATED DIBENZ(B,F) - 1,4-OXAZEPINES AND DIBENZO-(B,F)-1,4-THIAZEPINES

11-AMINOALKYLATED DIBENZ(B,F) - 1,4-OXAZEPINES AND DIBENZO-(B,F)-1,4-THIAZEPINES

机译:11-氨基烷基化的二苯并(B,F)-1,4-恶嗪和二苯并-(B,F)-1,4-噻嗪酮

摘要

Novel compounds of formula FORM:1105050/C2/1 wherein Z is O or S, R is C1- 3 alkyl and A is C1- 5 straight or branched alkylene, and acid addition salts thereof, are prepared by one of the following methods: (i) alkylation of the corresponding free or monoalkyl amine; (ii) reaction of a secondary amine with a reactive ester (e.g.halide) of a compound of formula FORM:1105050/C2/2 (iii) dehydrogenation of the corresponding 10,11-dihydro compound; or (iv) cyclization of a compound of formula FORM:1105050/C2/3 wherein Y is O, S or NH. Amides of the last formula above are prepared by reaction of a 2-amino-diphenyl ether or 2 - amino - diphenyl sulphide with a compound of formula X.CO.A.X, where X is halogen, to give the intermediate halo-substituted amide, which is then reacted with a secondary amine. 11 - Bromoethyl - dibenz(b,f) - 1,4 - oxazepine is prepared by bromination of the corresponding 11-methyl compound. Pharmaceutical compositions in conventional forms for oral or parenteral administration comprise an above novel compound and a carrier therefor.
机译:通过以下方法之一制备式的新型化合物及其酸加成盐,其中Z为O或S,R为C1-3烷基且A为C1-5直链或支链亚烷基。方法:(i)将相应的游离或单烷基胺烷基化; (ii)仲胺与式的化合物的反应性酯(例如卤化物)反应(iii)相应的10,11-二氢化合物脱氢; (iv)环化式的化合物,其中Y为O,S或NH。通过使2-氨基-二苯醚或2-氨基-二苯硫醚与式X.CO.AX的化合物(其中X为卤素)反应制得上述最后一个式的酰胺,得到中间体的卤素取代的酰胺,然后使其与仲胺反应。通过溴化相应的11-甲基化合物来制备11-溴乙基-苯甲酸(b,f)-1,4-氧杂ox平。用于口服或肠胃外给药的常规形式的药物组合物包含上述新型化合物及其载体。

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