摘要 |
The title compds.(I; R2 = fluoro, methoxy; R3 = H; R4 = chloro, bromo, iodo; R5 = H, halogeno; R6,R7,R8= H, halogeno, C1-4 alkyl, alkoxy; X = O, S) having enzyme inhibiting activities, were prepd. by hydrolysis of II (R1 = C1-4 alkoxy or III). Thus, 11.5 g Et 1,2-dinydro-1-oxo-phthalazin-4-ylacetic acid and 2.7 g sodium hydride were stirred at 60≦̸C for 1 hr in 125 ml DMF, and reacted with 15.0 g 4-bromo-3-chlorobenzyl bromide at 60≦̸C for 2 hr to give 7.3 g Et 2-(3-chloro-4-bromo benzyl)-1, 2-dihydro-1-oxophthalazin-4-ylacetate (m.p. 142-145).
|