| 摘要 |
Novel compounds of the Formula II, wherein R represents a hydrogen atom or an alkyl, trifluoromethyl-C1- 5 alkyl, aryl, aralkyl, cycloalkyl, alkylcycloalkyl, phenoxy, phenylthioalkyl, alkylphenoxy, phenylalkylthio or halophenylalkyl radical; each R1 represents a C1- 5 alkyl radical or the two symbols R1, together with the nitrogen atom to which they are attached, represent a 1-pyrrolidinyl, piperidino or morpholino radical; R2 represents a C1- 5 alkyl or benzyl radical; X represents a hydrogen or halogen atom or C1- 5 alkyl, C1- 5 alkoxy, trifluoromethyl or nitro radical or, taken together, two Xs on adjacent carbon atoms of the benzene ring may represent a 1,3-butadienylene chain; A represent a non-toxic; pharmacologically acceptable anion; m represents 1 or 2 and n represents an integer of from 1 to 5, are prepared by reacting compounds of the Formula IV with quaternizing agents of the formula AR2 wherein A represents the radical corresponding to the anion A-. Amines of the Formula IV may be prepared by reacting the appropriate (4-acylphenoxy-alkanoic) acids with formaldehyde and an acid addition salt of the appropriate secondary amine according to the Mannich reaction. <FORM:1079496/C2/1> <FORM:1079496/C2/2> 3-Fluoro-4-butyrylphenoxy) acetic acid may be prepared by reacting (3-fluorophenoxy) acetic acid with butyryl chloride and aluminium chloride. [4-(2-Methylenealkanoyl)phenoxy] acetic acids (see Specification 998,835) may be prepared by treating compounds of the Formula II with a weak base. Therapeutic compositions, with diuretic properties, for oral administration, comprise compounds of the Formula II with an inert carrier. |
