Etablissements Nativelle, S.a.

Georges Tsatsas

Georges V Foscolos

Evan E Costakis

The invention relates to new derivatives of spiro compounds represented by the general formula (I) ##STR1## wherein R is a hydrogen atom, a halogen atom, an alkyl group or an alkoxy group; R.sub.1 and R.sub.2 represent a hydrogen atom or an alkyl group or together form a nitrogen-containing heterocyclic ring; A is a&gt;CH.sub.2 group or a&gt;CO group; n is 4 or 5. These compounds can be prepared from .beta.-hydroxyacids by intramolecular rearrangement by the action of a strong acid, in order to form a .gamma.-spirolactone which is converted into an .alpha.-carboxy .gamma.-spirolactone to form the compounds of formula (I) using a Mannich reaction. As necessary, a reduction is then carried out. These compounds are useful medically, in particular, as an antidepressant, a stimulant, and a neuroleptic.

Process for preparing spiro derivatives

The invention relates to new derivatives of spiro compounds represented by the general formula (I) ##STR1## wherein R is a hydrogen atom, a halogen atom, an alkyl group or an alkoxy group; R.sub.1 and R.sub.2 represent a hydrogen atom or an alkyl group or together form a nitrogen-containing heterocyclic ring; A is a &gt;CH.sub.2 group or a &gt;CO group; n is 4 or 5. These compounds can be prepared from .beta.-hydroxyacids by intramolecular rearrangement by the action of a strong acid, in order to form a .gamma.-spirolactone which is converted into an .alpha.-carboxy .gamma.-spirolactone to form the compounds of formula (I) using a Mannich reaction. As necessary, a reduction is then carried out. These compounds are useful medically, in particular, as an antidepressant, a stimulant, and a neuroleptic.

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Athens, Greece

Georges Tsatsas