| 摘要 |
Compounds of formula <FORM:0993749/C2/1> wherein R11 is CONH2 or SO2X wherein X is alkyl, aryl or substituted alkyl or aryl, R12 and R13 are alkyl, aryl or aralkyl or substituted alkyl, aryl or aralkyl and Z1 completes a benzene ring which may be substituted, are prepared by reacting the appropriate 2-quinolone with phosphorus pentasulphide to give the 2-thioquinolone, quaternizing this with methyl iodide and then reacting this salt with a sulphonyl or carbonamido hydrazone. Specified compounds are those wherein R11 is carbamido, n-hexadecylsulphonyl and 4-carboxybenzenesulphonyl, R12 is methyl, isopropyl, trifluoromethyl, n-pentadecyl, phenyl and 4-chlorophenyl, R3 is methyl, isopropyl, n-heptyl, phenyl, benzyl, pentadecyl, and 4-(b -carboxyacryloylamino-phenyl) and the benzene ring may be substituted by methyl, methoxy, chloro or a b -carboxyacryloylamino radical. 1-methyl-4-pentadecyl-2-quinolone and 4-pentadecyl-6-methyl-2-quinolone are prepared by heating N-methyl palmitryl acetanilide or palmitoylacet-p-toluidide in strong sulphuric acid. The 2-thioquinones are prepared and quaternized as above and then reacted with 4-carboxyphenyl sulphonyl hydrazone. 1,4 - dimethyl - 6 - (b - carboxyacryloylamino)-2-quinolone-n-hexadecylsulphonyl hydrazone is prepared by reacting a quaternized 1-methyl-4-methyl-6-nitro-2-thioquinolone with n-hexadecylsulphonyl hydrazide to give 1,4-dimethyl-6 - nitro - 2 - quinolone - n - hexadecylsulphonylhydrazone, reducing this to the amino compound with Raney nickel, and reacting the amino compound with acetonitrile. 1 - methyl - 4 - [41 - (b - carboxyacryloylamino)-phenyl] - 2 - quinoline - n - hexadecylsulphonyl hydrazone is prepared by reducing 1-methyl-4-[41 - nitrophenyl] -2 -quinolone - n - hexadecylsulphonyl hydrazone to the amino compound which is reacted with acetonitrile. |
