| 摘要 |
Compounds useful as antiamebic agents are 1-(Ac1)-5-R-6-(Ac2O)-1,2,3,4-tetrahydroquinolines (I), where Ac1 is haloacetyl, dihaloacetyl or trihaloacetyl with halo being chloro or bromo, R is hydrogen, chloro or bromo, and Ac2 is hydrogen, Ac1, alkanoyl having from one to sixteen carbon atoms, benzoyl, 2(or 3)-thenoyl, 2(or 3)-furoyl or N-(lower-alkyl)carbamoyl. Said compounds are prepared: by reacting 1,2,3,4-tetrahydro-6-quinolinol with an acyl halide of the formula Ac1-halogen to produce 1-(Ac1)-1,2,3,4-tetrahydro-6-quinolinol having formula I where R and Ac2 are each hydrogen, Ac1 is defined as in formula I and halide is chloride or bromide; by reacting said 1-(Ac1)-1,2,3,4-tetrahydro-6-quinolinol with a chlorinating or brominating agent to produce the corresponding 1-(Ac1)-5-chloro(or bromo)-1,2,3,4-tetrahydro-6-quinolinol where Ac1 is defined as in claim 1; and, by reacting 1-(Ac1)-5-R-1,2,3,4-tetrahydro-6-quinolinol with an acylating agent providing Ac2 to produce 1-(Ac1)-5-R-1,2,3,4-tetrahydro-6-(Ac2O)quinoline having formula I where R is hydrogen, chloro or bromo, Ac1 is defined as in formula I and Ac2 is other than hydrogen as defined in formula I. |
