Process for the preparation of formylimidazoles

Details Process for the preparation of formylimidazoles Process for the preparation of formylimidazoles

C - Chemistry, Metallurgy

07

D

C07D 233/64 (2006.01) C07D 233/54 (2006.01) C07D 233/68 (2006.01) C07D 521/00 (2006.01)

Patent

CA 2274994

A novel process for the preparation of a formylimidazole of the general formula: (see formula I) or a tautomer thereof, is described in which R1 is hydrogen or alkyl, and R2 is hydrogen, halogen or alkyl, in which, in a first stage, an imidazole derivative of the general formula: (see formula II) or a tautomer thereof, in which R1 and R2 are as defined above, is converted, by introducing an amino protective group, into an imidazole derivative of the general formula: (see formula III) or a tautomer thereof, in which R3 is an amino protective group, which derivative is formylated in a second stage in the presence of an organometallic compound and a suitable electrophile to give an imidazole derivative of the general formula: (see formula IV) or a tautomer thereof, in which R1, R2 and R3 are as defined above, and then, in a third stage, the end product of the formula (I) is obtained by cleaving off the amino protective group.

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