| 摘要 |
1. Claims for the contracting States : BE, CH, DE, FR, GB, IT, LI, LU, NL, SE Compounds corresponding to the general formula I see diagramm : EP0172097,P8,F10 in which X denotes hydrogen, a halogen or a methyl, methoxy, methylthio or methylsulphonyl group, Y denotes hydrogen, a halogen or a methyl group at the 6-, 7- or 8-position, and R1 and R2, taken separately, each denote hydrogen or a methyl or ethyl group, or alternatively R1 and R2 together form a tetramethylene, pentamethylene, 3-methyl-3-azapentamethylene, 3-ethoxycarbonyl-3-azapentamethylene or 3-oxapentamethylene chain, as well as their pharmacologically acceptable addition salts. 1. Claims for the contracting State : AT Process for preparing compounds corresponding to the general formula I see diagramm : EP0172097,P9,F8 in which X denotes hydrogen, a halogen or a methyl, methoxy, methylthio or methylsulphonyl group, Y denotes hydrogen, a halogen or a methyl group at the 6-, 7- or 8-position, and R1 and R2, taken separately, each denote hydrogen or a methyl or ethyl group, or alternatively R1 and R2 together form a tetramethylene, pentamethylene, 3-methyl-3-azapentamethylene, 3-ethoxycarbonyl-3-azapentamethylene or 3-oxapentamethylene chain, which process is characterized in that either the quinoline of formula II see diagramm : EP0172097,P10,F2 is subjected to the action of an alpha-bromoacetophenone bearing the substituent X defined above, to obtain an ionic compound of formula III see diagramm : EP0172097,P10,F4 which is cyclized in the heated state in the presence of ammonium acetate and ferric chloride, or the 2-aminoquinoline of formula IV see diagramm : EP0172097,P10,F5 is subjected to the action of an alpha-bromoacetophenone bearing the substituent X defined above, thereby obtaining the compound of formula V see diagramm : EP0172097,P10,F6 which is subjected to a formylation to obtain the aldehyde of formula VI see diagramm : EP0172097,P10,F8 this compound is then reduced to an alcohol of formula VII see diagramm : EP0172097,P10,F9 which is converted to a nitrile of formula VIII see diagramm : EP0172097,P10,F1 which is hydrolysed to obtain the acid of formula IX see diagramm : EP0172097,P10,F3 and the latter is finally amidated by reacting it with an amine of formula R1-NH-R2 in which R1 and R2 are as defined above. |
