GB1047935A — Substituted piperazines and preparation thereof

USPTO Abstract

The invention comprises compounds of the formula <FORM:1047935/C2/1> and their pharmaceutically acceptable salts wherein n is 3 or 4; R1 and R2 are each H or C1- 6 alkyl groups; R3 and R4 are each H, C1- 6 alkyl or aralkyl groups; and R5 is a substituted acyl radical of the benzene type series or aromatic heterocyclic radical of at least 5 ring atoms or an acyl radical and the preparation thereof by reacting a compound of the formula <FORM:1047935/C2/2> with a compound R5-Z wherein Z is halogen, OH, O Alkyl, S Alkyl, SO Alkyl, SO2 Alkyl, sulphonato, nitro or an anhydride residue or by reacting a compound <FORM:1047935/C2/3> with a compound of the formula <FORM:1047935/C2/4> wherein Y is OH, OSO2 Alkyl or OSO2 Aryl, and if desired preparing from the products of either reaction the acid addition salts. 1 - (3 - Dimethylaminopropyl) -, 2,5 - dimethyl - 1 - (3 - dimethylaminopropyl) -, 1 - (4-dimethylaminobutyl) - and 1 - (4 - dimethylaminobutyl) - trans 2,5 - dimethyl - piperazines are prepared either by reacting a piperazine with a dialkylamino alkyl halide or by reducing the corresponding nitrile to give the primary amine then alkylating this with formic acid and formaldehyde. Pharmaceutical compositions comprise the compounds of the invention and a carrier therefor. The compositions, which inhibit the growth of protozoa, may be in a form suitable for enteral or parenteral administration.