Process for the preparation of piperidinylaminomethyl...

Details Process for the preparation of piperidinylaminomethyl... Process for the preparation of piperidinylaminomethyl...

C - Chemistry, Metallurgy

07

D

C07D 405/12 (2006.01) C07C 69/734 (2006.01) C07D 307/87 (2006.01) C07D 311/76 (2006.01) C07F 7/18 (2006.01)

Patent

CA 2323315

The present invention relates to a novel process for the preparation of a diastereomeric mixture of piperidinylaminomethyl trifluoromethyl cyclic ether compounds of formulae Ia and lb: (SEE FORMULA Ia) (SEE FORMULA Ib) and pharmaceutically acceptable salts thereof, wherein R1 is C1-C6 alkyl; R2 is C1-C6 alkyl, halo C1-C6 alkyl or phenyl or substituted phenyl; R3 is hydrogen or halo; m is zero, one or two, and wherein the mixture is highly enriched in the compound of formula Ia, and to novel processes for the preparation and purification of intermediate compounds useful in the preparation of compounds of formulae Ia and Ib. The compounds of the formulae Ia and Ib have substance P antagonist activities and are useful as medicine for treating diseases such as central nervous system disorders.

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