| 摘要 |
<p>NEW MATERIAL:A compound (salt) expressed by formula I [X1 and X2 are H or halogen; R1 is H or carboxy-protecting group; R2 and R3 are H, (substituted) alkyl, alkenyl, etc.; R4 is H, halogen, OH or R5O (R5 is alkyl, aryl, heterocyclic group, alkylsulfonyl, etc.), etc.]. EXAMPLE:Ethyl 9,10-difluoro-3-methyl-7-oxo-1H,3H,7H-pyrido[3,2,1- ij][3,1]benzoxazine-6-carboxylate. USE:A synthetic antimicrobial agent. PREPARATION:For example, o-hydroxymethylanilines expressed by formula II (X3' is H or halogen) are reacted with diethyl ethoxymethylenemalonate and then acylated to provide a compound expressed by formula III (R' is acyl; Et is ethyl), which is subsequently cyclized to afford a quinoline derivative. The resultant derivative is then hydrolyzed to provide 8-hydroxymethylquinolines expressed by formula IV (R'1 is alkyl), which are subsequently cyclized and hydrolyzed to afford the compound expressed by formula I.</p> |
