Process for the preparation of 1,3-diaza-spiro (4.4) non-1-en-4-one derivatives and 1-cyano-1-acylaminocyclopentane intermediates

• Main Authors: ZSUZSANNA NAD, ZOLTAN MAKOVI, CSABA HUSZAR, ILONA DERVALICSNE ZRINYI, AGNES KUNSZTNE KARASZ, ATTILA KIS-TAMAS, ENDRE KOLLAR, ISTVAN MESZAROS, ATTILA NEMETH, PETER ARANYOSI, ANTAL GAJARY, ERZSEBET BOGNAR, ZSUZSANNA CSETRINE HARI, KAROLY GYURE, ATTILA SUPIC, KATALIN DUBOVSZKI, LAJOSNE PALI
• Format: Patent
• Language: English
• Published: 16.02.1999
• Edition: 6

Process for the preparation of compounds of formula (I) wherein R means hydrogen atom, or C1-6 alkyl group, or C7-12 aralkyl group or phenyl group, characterised in that a) the compound of formula (III) is reacted with a compound of formula (IV) wherein X means halogen atom or C1-5 alkoxy group or hydroxyl group, and the resulting compound of formula (II) is transformed, in a reaction medium with pH above 7, into the compound of formula (I) or b) the compound of formula (III) is reacted with an anhydride of general formula (V) and the resulting compound of formula (II) transformed, in a reaction medium with pH above 7, into the compound of formula (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 if desired, the resulting compounds of formula (I), before or after isolation, are transformed into acid addition salts, or the compounds of formula (I) are liberated from their acid addition salts. Thus a process for the preparation of intermediates useful in synthesis of angiotensin II antagonists is disclosed.