PROCESS FOR THE PREPARATION OF 1,3-DIAZA-SPIRO (4.4) NON-1-EN-4-ONE DERIVATIVES AND 1-CYANO-1-ACYLAMINOCYCLOPENTANE INTERMEDIATES

摘要

Process for thepreparation of compoundsof formula (I) wherein Rmeans hydrogen atom, orC1-6 alkyl group or C7-12aralkyl group or phenylgroup, characterised in thata) the compound of formula(III) is reacted with acompound of formula (IV)wherein X means halogenatom or C1-5 alkoxy groupor hydroxyl group, andthe resulting compound offormula (II) is transformed,in a reaction mediumwith pH above 7, into thecompound of formula (I)or b) the compound of formula (III) is reacted with an anhydride of generalformula (V) and the resulting compound of formula (II)transformed, in a reaction medium with pH above 7, into the compound offormula (I), or c) a compound of formula (II) is transformed,in a reaction medium with pH above 7, into the compound of formula (I), and ifdesired, the resulting compounds of formula (I), before orafter isolation, are transformed into acid addidon salts, or the compounds offormula (I) are liberated from their acid addition salts. Thus aprocess for the preparation of intermediates useful in synthesis ofangiotensin II antagonists is disclosed.