| 摘要 |
Production of an acridine carboxamide of formula (I) or its salts comprises: (a) cyclising a compound of formula (II) by treatment with a Lewis acid in an organic solvent to give a compound of formula (III); and (b) treating either: (i) the compound (III) with a primary alkylamine of formula (IV); or (ii) the carboxylic acid obtainable by hydrolysing the compound (III) under basic conditions with an alkylamine of formula NH2(CH2)xY (IV) in the presence of a coupling agent to give a compound (I); and (c) optionally converting one compound (I) into another compound (I). R1,R2, R5,R6 = H, 1-6C alkyl, 1-6C alkoxy, aryloxy, aralkyloxy, halo, phenyl, CF3, NO2, NH2, N(R)2, NHCOR, NHCOOR, NHR4, OH, SH, SR or SR2; R4 = H, COR, SO2R, COPh, SO2Ph or 1-6C alkyl optionally substituted by OH or NH2; R = 1-6C alkyl; or R1+R2 or R5+R6 = methylenedioxy; x = 1-6; Y = N(R)2; R3 = 1-6C alkyl, aryl or aryl(1-3C)alkyl. |
