| 摘要 |
<p>Title cpds. of formula (I):- (where R1 is aryl, aralkyl, or cyclohexyl; and R2 is H, opt. substd. alkyl (opt. unsatd) or alkoxycarbonyl) have anti-inflammatory, analgesic, antiulcer antipyrtic, antihistaminic and CNS depressant activity. Cpds. (I; R2 = H) can be prepd. by reacting (I; R2 = H) with R'2X1 (R'2 is as R2 but not H; X1 = halogen or arylsulphonyloxy), X2CH2R3 (X2 = halogen; R3 = H or lower alkyl, R4 = CONH2, CN or alkoxycarbonyl), (R5O)2X3 (R5 is opt. substd. opt. unsatd. alkyl; X3 is CO, SO2 or COCO), CH2(X4)CH-R6 (X4 = O, OCOO or OSOO; R6 is H, lower alkyl, lower haloalkyl or aryl), or R7N2 (R7 = lower alkyl). (I; R2 = H) can be prepd. e.g. by reacting 2-aminonicotinamide with diethylcarbonate in the presence of NaOMe.</p> |
