| 摘要 |
Compounds of the general formula <FORM:1060463/C2/1> (wherein X represents a hydrogen, chlorine or bromine atom or a nitro, trifluoromethyl or methylsulphonyl group, R represents a hydrogen atom or a C1- 8 hydrocarbon group, Ar represents a thienyl group, or a phenyl group optionally substituted by a chlorine or fluorine atom or a methyl, methoxy or trifluoromethyl group, Z represents an alkylene, alkenylene or arylene radical of up to 8 carbon atoms optionally substituted by up to 4 further -COOM groups, n is 0 or 1 and M represents a hydrogen atom or the cation of an alkali metal, ammonium or amine salt) are prepared by (a) esterifying or transesterifying a compound of the formula <FORM:1060463/C2/2> (wherein R1 represents a hydrogen atom or a monocarboxylic acyl residue) with an appropriate polycarboxylic acid acylating agent (where a polycarboxylic acid halide is used the initial product is hydrolysed), (b) reacting a compound of the formula <FORM:1060463/C2/3> with a salt of the appropriate polycarboxylic acid or (c) reacting a compound of the formula <FORM:1060463/C2/4> with a polycarboxylic acid halide, hydrolysing the product and separating the required compound from the reaction mixture, optionally followed in each case by salt formation or conversion of a salt to the free acid. Some of the compounds of the invention are anticonvulsants and muscle relaxants, some are sedatives, some are tranquillizers without being sedatives and some have disinhibiting effects. They may be administered (e.g. by injection) in the form of pharmaceutical preparations containing them in association with a carrier. |
