2-/4-(ALKYLTHIO/-2,5-DIMETHOXYPHENYL) ETHYLAMINES AND THEIR HYDROGENMALEATES

The solution belongs to the synthetic pharmaceuticals sector. Its object is represented by 2-(4-(Alkylthio)-2,5-dimethoxyphenyl)ethylamines and their N-methyl- and N,N-dimethyl-derivatives, as well as their hydrogen maleates, while the alkyl is pentyl or heptyl. The substances according to the solution have a centrally inhibiting and hypothermic effect so they are potential tranquillizers; others antagonize the effects of reserpine in mice and rats, so they have anti-depressive effects. They are typically used due to their very strong antimicrobial effects, especially as regards Staphylococcus pyogenes aureus, so they can be considered as potential chemotherapeutics. Their preparation includes relevant (4-alkylthio-2,5-dimethoxyphenyl)acetonitriles which are reduced by aluminium hydride to primary amines according to the solution. These are subsequently methylated either to N-monomethyl derivatives or to N,N-dimethyl derivatives. Methylation into the first grade consists in N-formylation by mixing anhydride of acetic acid and formic acid and in the subsequent reduction by diborane. Methylation into the second grade is performed by boiling with formic acid and water formaldehyde. Neutralization by maleic acid transforms the products - bases - into crystalline hydrogen maleates, which are also part of the solution.