| 摘要 |
1451912 Piperazino-pyrimidopyridines DAINIPPON PHARMACEUTICAL CO Ltd 8 Aug 1973 [14 Aug 1972 19 Dec 1972 22 Dec 1972 26 Dec 1972 27 Dec 1972 25 May 1973 19 June 1973] 15392/76 Divided out of 1451911 Heading C2C The invention comprises compounds of the formula wherein R 1 is H, (C 1 -C 4 )alkyl, hydroxy (C 2 -C 4 )alkyl, benzyl, methoxybenzyl, phenyl, propargyl or carboxylic or carbonic acyl and R 3 is H or (C 1 -C 6 )alkyl, and salts thereof. They may be prepared by (1) reacting a compound of the formula wherein X is halogen, (C 1 -C 4 )alkylthio or (C 1 -C 4 )alkoxy, with a compound of the formula (2) compounds in which R 3 is H, hydrolysing a compound of Formula (I) wherein R 3 is (C 1 -C 6 ) alkyl; (3) compounds in which R 1 is H, hydrolysing a compound of formula wherein R<SP>1</SP> 1 is a (carboxylic or carbonic) acyl arylsulphonyl, vinyl, trityl or a group of formula wherein Z is halogen, (C 1 -C 4 )alkoxy, benzyloxy, alcoholic hydroxy, acyloxy, arylsulphonyloxy, (C 1 -C 4 )sulphonyloxy, s-aryldithiocarbonyloxy, (C 1 -C 4 )alkyldithiocarbonyloxy group or group forming with the -CH 2 CH 2 -moiety a tertiary or quaternary amino group; and (4) heating a compound of the formula wherein each of Y and Z are H or a group as defined above for Z, at least one of Y and Z being H. The compounds of Formula I have antibacterial activity and may be administered perorally, parenterally, enterally or locally in conventional forms. |
