Preparation of triazoles by organometallic addition to...

Organic compounds -- part of the class 532-570 series – Organic compounds – Nitrogen attached directly or indirectly to the purine ring...

Reexamination Certificate

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Reexamination Certificate

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11120739

ABSTRACT:
The invention provides a process for the preparation of a compound of the formula:or an acid addition or base salt thereof,whereinR is phenyl optionally substituted by 1 to 3 substituents each independently selected from halo and trifluoromethyl;R1is C1–C6alkyl; and“Het” is pyrimidinyl optionally substituted by 1 to 3 substituents each independently selected from C1–C4alkyl, C1–C4alkoxy, halo, oxo, benzyl and benzyloxy,comprising reaction of a compound of the formula:wherein R is as previously defined for a compound of the formula (I), with a compound of the formula:wherein R1and “Het” are as previously defined for a compound of the formula (I) and X is chloro, bromo or iodo, in the presence of zinc, iodine and/or a Lewis acid and an aprotic organic solvent: said process being optionally followed by conversion of the compound of the formula (I) to an acid addition or base salt thereof.

REFERENCES:
patent: 5364938 (1994-11-01), Dickinson et al.
patent: 5567817 (1996-10-01), Ray et al.
patent: 6586594 (2003-07-01), Butters et al.

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