ES251967A1 - Phenothiazine derivatives, and their preparation - Google Patents

Abstract

The invention comprises compounds of the general formula <FORM:0905692/IV (b)/1> (wherein X represents a hydrogen or halogen atom or a low molecular (i.e. C1-4) alkyl or alkoxy group, R1 and R2 represent low molecular alkyl radicals which can be bound to each other directly or through an oxygen atom or the nitrogen atom of a low molecular alkylimino, alkanoyloxyalkylimino or hydroxyalkylimino group, and n is a number from 1 to 3) and the preparation thereof by reacting a compound of the general formula <FORM:0905692/IV (b)/2> with a reactive ester of an aminoalcohol of the general formula <FORM:0905692/IV (b)/3> or by reacting a compound of the general formula <FORM:0905692/IV (b)/4> (wherein Y represents a reactive esterified hydroxy group) with a secondary amine HNR1R2 or by treating a compound of the general formula <FORM:0905692/IV (b)/5> with a low molecular alkylating agent. The products and their acid addition salts have antiallergic and sedative activity, whilst quaternary ammonium salts derived therefrom (e.g. by the action of aliphatic or araliphatic halides or sulphates) have a ganglioplegic action. The bases can also be made by reacting a compound of the second general formula above with phosgene, reacting the resulting 5-chlorocarbonyl compound with an amino-alcohol of the third general formula above, and heating the resulting ester of the general formula <FORM:0905692/IV (b)/6> until carbon dioxide is split off. Reactive esters of the fourth general formula above are prepared by reacting compounds of the second general formula above with haloethoxyethanols or a haloethoxyethoxyethanols and esterifying the resulting hydroxy compounds with strong inorganic or organic acids, e.g. halogen hydracids (by the action of inorganic acid halides), sulphuric acid or organic sulphonic acids.