PROCESS FOR THE PREPARATION OF (-)1BETA-ETHYL-1ALPHA- -(HYDROXYMETHYL)-1,2,3,4,6,7,12,12BALPHA-OCTAHYDRO-INDOLO [2,3-A]QUINOLIZINE AND INTERMEDIATES FOR THE PREPARATION THEREOF

摘要

During the preparation of a compound of the formula (I), 1-ethyl-2,3,4,6,7,12-hexahydro-indolo[2,3-a]quinolizine of the formula (II) reacts with an equimolar amount of formaldehyde, and, the obtained 1-ethyl-1-(hydroxymethyl)-1,2,3,4,6,7- -hexahydro-12H-indolo[2,3-a]quinolizine of the formula (III) reacts with a cracking agent (-)-L-dibenzoyltartaric acid in an amount lesser than the equimolar amount. Thus obtained 1beta- -ethyl-1alpha-(hydroxymethyl)-1,2,3,4,5,6,7-hexahydro-12H- -indolo[2,3,-a]quinolizin-5-ic salt of the general formula (IV)-wherein X- denotes a residual of the optically active (-)-L-dibenzoyltartaric acid is reduced and the free base of the formula (I) is liberated. 1-ethyl-1-(hydroxymethyl)-1,2,3,4,6,7- -hexahydro-12H-indolo[2,3-a)quinolizine of the formula (III) and 1beta-etyl-1alpha-(hydroxymethyl)-1,2,3,4,6,7-hexahydro-12H- -indolo[2,3-a]quinolizin-5-ic salt of the formula (IV), wherein X- denotes a residual of the optically active (-)-L-dibenzoyltartaric acid, are intermediates for the preparation of said compound.