| 摘要 |
<p>The present invention relates to a process for the preparation of 5-methyl-6-trifluoromethyl-indoline which is a key intermediate in the preparation of compounds having 5-HT2C receptor antagonist activity. The reaction sequence starts from 1-chloro-2-nitro-4-trifluoromethyl-benzene (VII) via cyano-(2-nitro-trifluoromethylphenyl)acetic acid benzyl ester (VI), 6-trifluoromethyl-indole (V), 6-trifluoromethyl-indoline (IV), 1-benzyl-6-trifluoromethyl-indoline (III), 1-benzyl-5-bromo-6-trifluoromethyl-indoline (II) and 1-benzyl-5-methyl-6-trifluoromethyl-indoline (I). In a further aspect the present invention also relates to the compounds of formulae (I), (II), (III), (IV) and (VI).</p> |
