Sanofi-aventis

Kálmán Simon

Lajos T Nagy

Andrea Sántáné Csutor

Attila Simon

Gergely Héja

Csaba Gönczi

Tiborné Szomor

István Hermecz

Györgyné Szvoboda

Éva Csikós

Árpád Illár

Ágota Smelkóné Esek

The invention relates to a process for the preparation of spiro[(4-cyclohexanone)-[3H]indol]-2'[1&#x2032;H]-one derivatives of the general formula Iwherein Rand Rindependently stand for hydrogen, Calkyl, Calkoxy, Calkylthio, Cpolyfluoroalkyl, Cpolyfluoroalkoxy, Ccycloalkyloxy, Ccycloalkylthio, phenoxy, benzyloxy or nitro group&#x2014;,characterized by reacting an indolin-2-one derivative of the general formula IIwherein Rand Rare as defined above&#x2014;with a compound capable for introducing a protective group, selected from 2-tetrahydropyranyl, 1-diethoxy-methylene or Calkoxycarbonylethyl group, coupling the compound of general formula III,thus obtained&#x2014;wherein Rand Rare as defined above and A stands for a protective group, selected from 2-tetrahydropyranyl, 1-diethoxy-methylene or Calkoxycarbonylethyl group&#x2014;with an acrylic acid Cester, cyclizing the resulting compound of the general formula IVwherein R, Rand A are as defined above, Rstands for Calkyl group&#x2014;, eliminating the &#x2014;COORgroup and the A protective group of the keto-ester of general formula Vwherein R, R, Rand A are as defined above, optionally without isolation of the compounds of the general formulae IV

Process for the preparation of spiro[(4-cyclohexanone)-[3]indol]-2'[1&#x2032;H]-one derivatives

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Budapest, Hungary

Kálmán Simon