Process for the preparation of piperidinylidene derivative

Details Process for the preparation of piperidinylidene derivative Process for the preparation of piperidinylidene derivative

C - Chemistry, Metallurgy

07

D

C07D 211/70 (2006.01)

Patent

CA 2236127

Disclosed is a process for economic, safe and simple production of a 2-phenyl-2-(2'-piperidinylidene)acetate derivative at a reduced number of steps in a high yield, which comprises allowing 2,3,4,5-Tetrahydro-6-methoxypyridine and a benzyl cyanide derivative represented by the following general formula (2): (see fig.I) wherein R1 represents a hydrogen atom, a lower alkyl group, a lower alkoxy group, a halogen atom or an amino group, to undergo condensation reaction in the presence of an organic base such as 1,8-diazabicyclo[5.4.0]-7-undecene or a transition metal complex as a catalyst to produce a 2-phenyl-2-(2'-piperidinylidene)acetonitrile derivative represented by the following general formula (4): (see fig.II) wherein R1 is as defined above; and the wavy line indicates a geometrical isomer, and then reacting with an alcohol in the presence of hydrogen chloride.

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