专利名称：5-aminoalkyl-5, 7-dihydro-6h-dibenzo [d, f] [1, 3] diazepin-6-one compounds
发明人：DAVOLL JOHN
申请号：US33772664
申请日：19640115
公开号：US3264284A
公开日：
19660802
reactive diluent
专利内容由知识产权出版社提供
摘要：The invention comprises 5-aminoalkyl-5,7-dihydro - 6H - dibenzo[d,f]
[1,3]diazepin-6-one compounds of the formula and acid addition salts thereof; where n is 2 or 3; R represents a hydrogen atom or a methyl, ethyl or benzyl radical; R1 represents a methyl or ethyl radical; and R2 and R3 are the same and represent hydrogen or halogen atoms or methyl radicals. Compounds of the above formula where R is a methyl, ethyl or benzyl radical are prepared either by reacting an alkali metal salt of a compound of the formula with an aminoalkylhalide of the formula or, alternatively, by reacting a 2-amino-21-(aminoalkylamino -biphenyl compound of the formula with a reactive derivative of carbonic acid, e.g. urea, phosgene, ammonium carbamate or an alkali metal salt of cyanic acid; where R4 represents a methyl, ethyl or benzyl radical, X represents a halogen atom and n. R1, R2 and R3 have the abovementioned significance. Compounds of Formula I in which R represents a hydrogen atom are prepared by hydrogenolysis of the corresponding benzyl compound. Starting materials of formula II may be prepared by reacting a diaminobiphenyl compound of the formula with urea at a temperature between 180 DEG C. and 210 DEG C. until evolution of ammonia ceases. The alkali metal salts may be prepared by heating the dibenzo diazepinone compound with an alkali
metal amide or hydride at the reflux temperature of the reaction solvent until salt formation is complete. Starting materials of formula III may be prepared by reduction of biphenyl compounds of the formula which may in turn be prepared by the amino-alkylation of compounds of the formula or a N-formyl derivatives thereof with an aminoalkylhalide of the formula 2,21 - Diaminobiphenyl compounds of formula IV may be prepared by catalytic reduction of the corresponding 2,21-dinitrobiphenyl compounds. 2 -Nitro - 21 - aminobiphenyl compounds of formula VI may be prepared by selective reduction of the corresponding 2,21-dinitrobiphenyl compounds. Pharmaceutical compositions for oral or parenteral administration comprise a compound of the invention together with a pharmaceutical diluent and/or excipient. The compositions are active as central nervous system stimulants and diuretic agents and may be formulated as tablets, pills, sachets, packaged or encapsulated powders, solutions or suspensions.
申请人：PARKE, DAVIS & COMPANY
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