| 摘要 |
Title compds. (I; A = a, b, c; R5 = H, CF3, halogen; R6 = H, CF3, halogen, lower alkyl; R2 = H; R3 = lower alkyl; R2R3 = (CH2)3, CH:CHCH2: R4 = Me, Et, iso-Pr) were prepd. by reaction of II (X = eliminating group) and III. Thus, 24 g 5-fluoroisatic acid anhydride was treated with 11.8 g sarcosine in 140 ml DMSO, and stirred at 100oC for 1.5 hr to give 7-fluoro-3,4-dihydro-4-methyl-2H-1,4-benzodiazepin-2,5(1H)-di-one(m.p. 262-263oC). I had a diazepam antagonist ED50 at 5.8mg/kg orally in mice.
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