| 摘要 |
1466932 Pyrimidobenzodiazepines BRISTOL-MYERS CO 16 April 1974 [16 April 1973 25 Feb 1974] 16510/74 Heading C2C Pyrimidobenzodiazepines are prepared by the following routes (R,R<SP>3</SP>=H, C 1-6 alkyl, R<SP>5</SP>Ph(CH 2 ) n ; n=1-4; R<SP>5</SP>=H, F, Cl, Br, CF 3 , C 1-6 alkyl or alkoxy; R<SP>2,4</SP>=H, F, Cl, Br, CF 3 , NO 2 , C 1-6 alkyl or alkoxy; X=halogen; Y=di(C 1-6 alkyl)amino, C 3-6 cycloalkylamino, benzylamino, phenethylamino, di(C 1-6 alkyl)amino(C 1-6 alkyl)amino), optionally followed by salt formation. The 5,6- dihydro - 11H - pyrimido[4,5-b][1,4]benzodiazepines may alternatively be prepared by cyclizing a 5-(o-aminobenzylamino)-4-alkoxypyrimidine with a strong base in the presence of a solvent, optionally followed by introduction of an 11-substituent. The preparation of benzyl 4-ethoxy-5-pyrimidylcarbamate, 5 - amino - 4 - ethoxypyrimidine, 4 - ethoxy - 5 - (o - nitrobenzalamino)pyrimidine, 4 - ethoxy - 5 - (o - nitrobenzylamino)pyrimidine, 5 - (o - aminobenzylamino) - 4 - ethoxypyrimidine, N,5 - dimethylisatoic anhydride and methyl N,5-dimethylanthranilate is described. The above compounds possess antihypoxic, hypothermic, antipyretic and anti-inflammatory activity, and may be administered in the form of pharmaceutical preparations containing them in association with a carrier.
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