| 摘要 |
1445465 Aldol products of quinoxaline-2- carboxaldehyde-1,4-dioxide PFIZER Inc 19 Oct 1973 [3 Nov 1972] 48944/73 Heading C2C Novel compounds I in which R is hydrogen or methyl X is -CN, - COCH 3 , -CONR 1 R 2 , -CONR(CH 2 ) n R 3 or -COOR 4 (in which R 1 , R 2 and R 4 are hydrogen, methyl or ethyl and R 3 is -OH or -N(CR 3 ) 2 , n is 2 or 3), Y is hydrogen or X, Z 1 is hydrogen, chloro, methyl, methoxy, -SO 2 NH 2 , or -SO 2 N(CH 3 ) 2 , Z 2 is hydrogen, chloro or methyl with Z 1 and Z 2 being in the 6- or 7- position and with the proviso that when Z 2 is chloro or methyl, Z 1 is chloro or methyl and the alkali metal, ammonium and amine salts thereof when X and/or Y is -COOH and the acid addition salts thereof when R 3 is N(CH 3 ) 2 are prepared by reaction of the appropriate 2-quinoxaline carbonaldehyde-1,4-dioxide with an active methylene nucleophile in a Knocveragel reaction without elimination of water. p - Hydroxy - 2 - quinoxalinepropionamide N<SP>1</SP>,N<SP>4</SP> dioxide and the corresponding 3-methyl derivative are prepared by decarboxylating the corresponding malonamic acid. Compounds I are active against pathogenic microorganisms and may be used in watertreatment, slime control, paint and wood preservation and as disinfectants. Compounds I are also effective against gram-negative and gram-positive bacteria and are useful as growth promotants and may form with a suitable vehicle a pharmaceutical composition for administration orally or parenterally or may be added to an animal feed or drink. |
