| 摘要 |
NEW MATERIAL:The compound of formula I[R<1> is cyclopropyl, thienyl, etc., which may be substituted with halogen, etc.; R<2> is (substituted) 5-9-membered heterocyclic residue; R<3> is H, OH, etc.; R<4> is H, amino, etc.; X is halogen; when R<4> is H, R<3> is not H or halogen] and its salt. EXAMPLE:9-Cyclopropyl-5-methyl-6-fluoro-7-(4-methyl-1-piperazinyl)-2,3 ,4,9- tetrahydroisothiazolo[5,4-b]quinoline-3,4-dione. USE:An antibacterial agent. PREPARATION:The objective compound can be produced by (1) halogenating a compound of formula II (R<2>' is R<2>, etc.; X<2> is X), (2) reacting with a compound of formula III (R<5> is -COR<10>, etc.; R<10> and R<6> are lower alkyl), (3) removing the group R<5> from the produced compound of formula IV, (4) successively reacting with a compound of formula R<1>-N=C=S and a compound of formula R<7>-X<3> (R<7> is R<6>; X<3> is X), (5) cyclizing and then oxidizing the resultant compound of formula V and (6) reacting the resultant compound of formula VI with NH2OSO3H. |
