Procédé de préparation de sulfamides

The invention comprises sulphonamides of the formula in which A is a C2- 5 alkylene group or a group of the formula R1 is a phenyl, lower alkylphenyl, lower alkoxyphenyl, aminophenyl, hydroxyphenyl, dihalophenyl, di-lower alkylphenyl, di-lower alkoxyphenyl or methylenedioxy-phenyl group; R2 is hydrogen or lower alkyl; R3 and R4 are hydrogen, lower alkyl or together with the nitrogen atom form an N-pyrrolidinyl, N-piperidyl, N-piperazinyl, N1-lower alkyl-N-piperazinyl, or N1-(hydroxy-lower alkyl)-N-piperazinyl groups and R5 is hydrogen or lower alkyl (the word "lower" indicating a group of 1-6 carbon atoms). The compounds are prepared by (a) reacting a phenylalkylamine with sulphamide; (b) reacting an N-lower alkyl- or N-acyl - chlorosulphonylphenylalkyl (or -cyclopropyl)amine with ammonia or the appropriate amine, followed by hydrolysis of the N-acyl (e.g. N-acetyl or N-formyl group if desired; or (c) reacting a phenylalkyl- or phenylcyclopropylamine with a sulphamoyl chloride. Compounds wherein R3 or R4 is an alkyl group may be prepared by treating the N1-unsubstituted phenylalkyl- (or phenylcyclopropyl) sulphonamide with an alkylating agent. The piperazino and N1-hydroxyalkyl piperazino are made via the corresponding derivatives bearing protective acyl groups, e.g. the N1-acyl-piperazino and N1 - acyloxyalkyl - piperazino compounds. The phenylcyclopropysulphamide products may be obtained in cis, trans and d or l optical isomeric forms. N-Lower alkyl- or N-acyl-N-chlorosulphonyl amines used as starting materials in method (b) are made by reacting an N-lower alkylamine or sodio derivative of an N-acylamine, with sulphuryl chloride. Pharmaceutical preparations having tranquilizing activity comprise the above compounds of the invention in association with a carrier suitable for oral or parenteral administration, e.g. as solutions in peanut oil, olive oil, sesame oil or water, or tablets, powders, capsules, troches or lozenges.