Sanofi-synthelabo

Zolt&aacute;n Makovi

Attila Supic

Istv&aacute;n M&eacute;sz&aacute;ros

&Aacute;gnes Kunsztn&eacute; K&aacute;r&aacute;sz

Antal Gaj&aacute;ry

Attila Kis-Tam&aacute;s

Erzs&eacute;bet Bogn&aacute;r

Zsuzsanna N&aacute;d

Csaba Husz&aacute;r

Attila N&eacute;meth

P&eacute;ter Aranyosi

K&aacute;roly Gy&uuml;re

Lajosn&eacute; P&aacute;li

Endre Koll&aacute;r

Zsuzsanna Csetrin&eacute; H&aacute;ri

Katalin Dubovszki

Bertrand Castro

M&aacute;ria Bakonyi

Edit Bai N&eacute;e T&aacute;llai

Piroska Jobb

Ilona Dervalicsne Zrinyi

Marianna Csat&aacute;ri N&eacute;e Nagy

Erzs&eacute;bet Moln&aacute;r N&eacute;e Bak&oacute;

Ilona Dervalicsn&eacute; Zr&iacute;nyi

Intermediates and process for the preparation thereof

Process for the preparation of compounds of formula (I) wherein R means hydrogen atom, or C,alkyl group, or C,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 C,alkoxy group or hydroxyl group and the resulting compound of formula (II) is transformed in the presence of an oxidising agent 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 the presence of an oxidising agent, in a reaction medium with pH above 7, into the compound of formula (I), or c) a compound of formula (II) is transformed in the presence of an oxidising agent, 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.

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

Process for the preparation of compounds of formula (I) wherein R means hydrogen atom, or C,alkyl group, or C,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 C,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.

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

Growing community of inventors

Budapest, Hungary

Zoltán Makovi

Growing community of inventors

Budapest, Hungary

Zolt&aacute;n Makovi

Zoltán Makovi