Production of imidazole derivatives and novel intermediates...

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

Reexamination Certificate

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Reexamination Certificate

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06951944

ABSTRACT:
An improvement in the production of imidazole derivatives including histamine H3agonist immepip and histamine H3antagonist VUF4929. Desired imidazole derivatives can be easily obtained in high yield by using novel intermediates represented by the general formula (I): (I) wherein R1is an amino-protecting group; R2and R3are each independently hydrogen, lower alkyl, or hydroxylated lower alkyl; R4is lower alkyl, halogenated lower alkyl, or substituted or unsubstituted phenyl; and A is C1-3alkylene

REFERENCES:
patent: 6100264 (2000-08-01), Aloup et al.
patent: 93/12107 (1993-06-01), None
patent: 95/06037 (1995-03-01), None
Synthesis (1988); No. 9: 735-739.
Vollinga et al., “A New Potent and Selective Histamine H3Receptor Agnoist, 4-(1H-Imidazol-4-ylmethyl)piperidine”, Journal of Medicinal Chemistry (1994); 37: 332-333.
Harusawa et al., “An Efficient and Convenient Synthesis of 4-Vinylimidazoles Using Novel Homer-Wadsworth-Emmons (HWE) Reagent: Synthetic Studies Toward Novel Histamine H3-Ligands”, Synthesis (2002); No. 8: 1072-1078.

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