4-aryl-1-phenylalkyl-1,2,3,6-tetrahydropyridines having...

C - Chemistry – Metallurgy – 07 – D

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C07D 211/70 (2006.01) A61K 31/44 (2006.01) C07B 37/04 (2006.01) C07D 211/52 (2006.01) C07D 401/04 (2006.01)

Patent

CA 2420620

Compounds of formula (t): (see formula I) in which the benzene can optionally be substituted and X' is a phenyl optionally monosubstituted or polysubstituted by a halogen, CF3, (C1-C4) alkyl, (C1-C4) alkoxy, cyano, amino, mono- or di- (C1-C4) alkylamino, (C1-C4) acylamino, carboxyl, (C1-C4) alkoxycarbonyl, aminocarbonyl, mono- or di-(C1-C4) alkylaminocarbonyl, amino (C1-C4) alkyl, hydroxy (C1-C4) alkyl or halogeno(C1-C4)alkyl are prepared by reacting a compound of formula (w): (see formula II) in which the benzene can optionally be substituted and L' is a leaving group, with a benzeneboronic acid of the formula X'- B(OH)2, in which X' is as defined above, in the presence of a palladium salt, a strong base and a phase transfer agent, in an aqueous medium. The compounds are useful as intermediates in the preparation of certain novel 4-substituted 1- phenylalkyl-1,2,3,6-tetrahydropyridines having neurotrophic and neuroprotective activity.

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