Process for preparing 2-phenyl-3-aminopyridine, substituted...

C - Chemistry – Metallurgy – 07 – D

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C07D 213/73 (2006.01) C07D 213/75 (2006.01) C07D 401/00 (2006.01) C07D 405/00 (2006.01) C07D 409/00 (2006.01) C07D 413/00 (2006.01) C07D 417/00 (2006.01)

Patent

CA 2308817

A process for preparing 2-phenyl-3-aminopyridine, and substituted phenyl derivatives and salts thereof. A compound of the formula (see formula III or VIII) is reacted with a compound of the formula (see formula IV) in a reaction inert solvent in the presence of a base and a palladium catalyst to obtain a compound of the formula (see formula V or X) Preferably, the compound of formula III or VIII is prepared by reacting a compound of the formula (see formula I) with a compound of the formula (see formula II) or ArCHO VII in a reaction inert solvent. The compound of formula V is preferably deprotected in aqueous acid to obtain a salt of compound X. In the above reactions, R1 is optionally substituted alkyl, cycloalkyl or aryl; X is halo; Ar is optionally substituted aryl; Z is H, halo, alkyl or optionally substituted alkoxy; R3 and R4 are independently H or alkyl or are taken together to form a ring; and Y is halo or -OC(O)R2, wherein R2 is optionally substituted alkyl, cycloalkyl or aryl.

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