Process for the preparation of formylimidazoles

Organic compounds -- part of the class 532-570 series – Organic compounds – Heterocyclic carbon compounds containing a hetero ring...

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5483164, 5483185, C07D23356, C07D23358, C07B 4106

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061275484

ABSTRACT:
A process for the preparation of formylimidazoles of the general formula: or its tautomers, in which R.sup.1 is hydrogen or alkyl, and R.sup.2 is hydrogen, halogen or alkyl. In a first stage, an imidazole derivative of the general formula: ##STR1## or its tautomers, in which R.sup.1 and R.sup.2 are as defined above, is converted, by introducing an amino protective group, into an imidazole derivative of the general formula: ##STR2## or its tautomers, in which R.sup.3 is an amino protective group. Such 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: ##STR3## or its tautomers, in which R.sup.1, R.sup.2 and R.sup.3 are as defined above. Then, in a third stage, the end product of the formula I is obtained by cleaving off the amino protective group.

REFERENCES:
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patent: 4924000 (1990-05-01), Hesse et al.
patent: 5521206 (1996-05-01), Muller et al.
patent: 5565577 (1996-10-01), Mokhallalatz et al.
patent: 5917051 (1999-06-01), Heveling et al.

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