Verfahren zur Herstellung von Phenylcyclopropyl-derivaten

摘要

The invention comprises compounds of general formula: wherein R is hydrogen, lower (1-8C) alkyl, lower alkenyl, phenyl-lower alkyl, nuclear substituted phenyl-lower alkyl, cycloalkyl, cycloalkyl-lower alkyl, hydroxy-lower alkyl, halo-lower alkyl, dicyclic hydroxy methyl, mono- or di-amino-lower alkyl, (halophenoxy)-lower alkyl, (mercapto)-(amino)-substituted lower alkyl, (alkyl-mercapto)-(amino)-substituted lower alkyl, (hydroxy)-(amino)-substituted lower alkyl, o -carboxy-(amino)-lower alkyl, a nitrogen-containing heterocyclyl group, an o -(nitrogen-containing heterocyclyl)-(amino)-lower alkyl group, or an o -(nitrogen-containing heterocyclyl)-lower alkyl group; trans isomers are preferred: and the process of reacting a compound of formula: with a compound of formula: in the presence of dicyclohexylcarbodiimide to yield a product of formula: wherein R1 is mono- or di-amino-lower alkyl, (mercapto)-(amino), substituted lower alkyl, (alkyl-mercapto)-(amino)-substituted lower alkyl, (hydroxy)-(amino)-substituted lower alkyl, an o -carboxy-(amino)-lower alkyl group, a nitrogen-containing heterocyclyl group, or an o -(nitrogen-containing-heterocyclyl) - (amino) - lower alkyl group. Other processes exemplified use as starting material acid halides which are reacted with the phenylcyclopropylamine; N-(trans-2-phenylcyclopropyl)-2-piperidino-acetamide is prepared by reacting the chloroacetamide with piperidine. Pharmaceutical compositions are mentioned which comprise compounds I together with suitable carriers for administration to humans and animals. Oral administration and solid (tablets, capsules) and liquid carriers are mentioned. The compounds inhibit monoamine oxidase and are used in depression, angina pectoris and arthritis.