| 摘要 |
PURPOSE:To obtain a 5-azaphthalide deriv. selectively in a high yield by using a pyridinemonocarboxylic acid chloride deriv. as the intermediate, converting it into a ketocarboxylic acid, and reacting the acid with an amino-substd. arom. ring. CONSTITUTION:This 5-azaphthalide driv. is produced by reacting a pyridine-3,4- dicarboxylic anhydride deriv. of formula I with an alcohol represented by R<1>OH, reacting the resulting pyridinemonocarboxylic acid deriv. of formula II with a chlorinating agent, and using the resulting acid chloride of formula III as the intermediate. The acid chloride is reacted with a compd. of formula IV, etc., to give a ketocarboxylic ester of formula V, etc., which is hydrolyzed in the presence of an alkali and then reacted with a compd. of formula VI, etc., giving the objective 5-azaphthalide deriv. of formula VII, etc. In those formulas, R<1> is a lower alkyl; R<2> to R<7> are each H, etc.; R<8> and R<9> are each the same as R<2> or R<3>; R<10> is the same as R<4>; R<11> and R<12> are each the same as R<5> or R<6>; and R<13> is the same as R<7>. |
