| 摘要 |
The invention relates to a process for the preparation of spiro[(4-cyclohexanone)-[3H]indol]-2'[1'H]-one derivatives of the general formula I wherein R<1 >and R<2 >independently stand for hydrogen, C1-4alkyl, C1-4alkoxy, C1-4alkylthio, C1-4polyfluoroalkyl, C1-4polyfluoroalkoxy, C3-7cycloalkyloxy, C3-7cycloalkylthio, phenoxy, benzyloxy or nitro group-, characterized by reacting an indolin-2-one derivative of the general formula II wherein R<1 >and R<2 >are as defined above-with a compound capable for introducing a protective group, selected from 2-tetrahydropyranyl, 1-diethoxy-methylene or C1-4alkoxycarbonylethyl group, coupling the compound of general formula III, thus obtained-wherein R<1 >and R<2 >are as defined above and A stands for a protective group, selected from 2-tetrahydropyranyl, 1-diethoxy-methylene or C1-4alkoxycarbonylethyl group-with an acrylic acid C1-4ester, cyclizing the resulting compound of the general formula IV wherein R<1>, R<2 >and A are as defined above, R<3 >stands for C1-4 alkyl group-, eliminating the -COOR<3 >group and the A protective group of the keto-ester of general formula V wherein R<1>, R<2>, R<3 >and A are as defined above, optionally without isolation of the compounds of the general formulae IV
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