C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
260/239.5
C07D 487/04 (2006.01)
Patent
CA 1164457
ABSTRACT OF THE DISCLOSURE The present invention provides compounds of formula Image where R1, R2 and R3 independently represent hydrogen, halogen or C1-4haloalkyl, R6 is C1-6alkyl, C3-7cycloalkyl or C3-7cycloalkylC1-6alkyl , and Q is -OH or -NH2. These compounds, which are useful as intermediates for the preparation of compounds of formula (I): Image wherein R1, R2, R3 and R6 are defined above; and in which R5 is a group of the formula Image where R9 is hydrogen, C1-14 alkyl, C3-7 cycloalkyl, C3-7 cycloalkyl, C1-4 alkyl, C1-4 haloalkyl, C2-4 alkenyl, C1-4 alkanoul, benzyl, cyano or optionally substituted phenyl, where R10 is hydrogen, C1-4 alkyl or optionally substituted phenyl, and where n is 0 or 1; are prepared by ring closing a compound of formula Image where Z is CN, COOH or COOR12, R12 being a C1-4 alkyl group. The compounds of formula (I) as defined above have neuroleptic, sedative, relaxant, anxiolytic or anti-emetic properties, and low toxicity, and are useful in the treatment of disorders of the central nervous system.
433655
Chakrabarti Jiban K.
Hotten Terrence M.
Gowling Lafleur Henderson Llp
Lilly Industries Limited
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