摘要 |
<p>Spiro((4-cyclohexanone)-(3H)indol-2'(1'H)-one derivatives (I) are prepared via new intermediates. Preparation of spiro((4 cyclohexanone)-(3H)indol-2'(1'H)-one derivatives of formula (I) comprises: (a) reacting an indol-2-one derivative of formula (II) with a compound capable of introducing a protective group to give (III); (b) coupling (III) with an acrylic acid 1-4C ester to give (IV); (c) cyclizing (IV) to give (V); (d) eliminating COOR 3>and the A protective group from (V) to give (I). [Image] R 1>, R 2>H, 1-4C alkyl, 1-4C alkoxy, 1-4C alkylthio, 1-4C polyfluoroalkyl, 1-4C polyfluoroalkoxy, 3-7C cycloalkyloxy, 3-7C cycloalkylthio, phenoxy, benzyloxy or NO 2; R 3>1-4C alkyl; A : a protective group. Independent claims are included for new compounds (III), (IV), (V) and (VI). [Image].</p> |