Process for the preparation of substituted piperidine-epoxides

C - Chemistry – Metallurgy – 07 – D

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C07D 211/42 (2006.01) C07D 211/52 (2006.01) C07D 211/70 (2006.01) C07D 211/74 (2006.01) C07D 491/04 (2006.01) C07D 491/044 (2006.01)

Patent

CA 2279817

The present invention concerns a process for the preparation of a compound of formula 1 or a salt thereof (see formula I) characterised in that the process comprises a) epoxidation of a compound of formula 2 or a salt thereof (see formula II) in which formulae A is arylene; R1 is -C*R3R4R5; R2 is -O-alkyl, -O-cycloalkyl, -O-alkenyl, -O-aryl, -O-aralkyl, -O-aralkoxyalkyl, -O-alkylsulfonyl, -O-arylsulfonyl, chlorine, bromine or iodine; R3 is hydrogen; R4 is aryl; R5 is alkyl, cycloalkyl, aryl, alkoxyalkyl or hydroxyalkyl; and, wherein C* is an asymmetric carbon atom; b) optionally followed by isolation of the desired stereoisomer.

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