摘要 |
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-indole (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). |
申请人 |
SMITHKLINE BEECHAM PLC;ANDREWS, IAN, PHILIP;FARUK, EROL, ALI;GRAY, MATTHEW;HOSSNER, FRANK;KITTERINGHAM, JOHN;PAKNOHAM, SANDRA, JANE;VOYLE, MARTYN |
发明人 |
ANDREWS, IAN, PHILIP;FARUK, EROL, ALI;GRAY, MATTHEW;HOSSNER, FRANK;KITTERINGHAM, JOHN;PAKNOHAM, SANDRA, JANE;VOYLE, MARTYN |