| 摘要 |
8-Fluoroalkyl-1,2-dihydro-4H-pyrrolo(3,2,1-ij)quinoline-4-ones and related cpds. of formula (I) and their intermediates (II) are new. In the formula, R1-2 independently are H or 1-4C alkyl with the condition that when R1 is alkyl then R2 is H, or (m)ethyl, or R1 and R2 together are (a) -CR6R8-CR7R9-, (b) -CHR10-CHR11-CHR12 or (c) -(CH2)4-; R6,R7 independently are H or methyl; R8,R9 independently are H or 1-4C alkyl or R8 and R9 together are (CH2)4- with the conditions (I) at least one of R6-9 is H (2) the total C atoms of R6-9 =6; R10-12 independently are H or (m)ethyl or R11 together with R10 or R12 form -(CH2)4- with the condition that at least one of R10-12 is H; R3 is H, methyl, F, Cl, Br, No, NH2 or OH; R4 is H or 1-4C alkyl; R5 is H, acyl or 1-6C alkyl; Ra and Rb independently are CF3, CF2Cl or CF2H; with the condition that both Ra and Rb is not = CF3, except when R5 is benzyl (sic). When R5 is H the metal salts with the hydroxy gp. are also claimed. Novel cpds. of formula (II) are those in which R1 and R2 together form a Gp. (a), (b) or (c). The cpds. are antihypertensives which act by direct peripheral vasodilation and do not have undesirable side-effects such as the CNS activity of alpha-methyldopa and clonidine. |
