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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C544S334000

Reexamination Certificate

active

06946555

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.

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patent: 440372 (1991-08-01), None
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Cram and Hammond , “Organic Chemistry” McGraw-Hill Book Co., NY (1964) 2nd Ed. pp 565-67.
Dickinson, R. P., et al., Bioorganic and Medicinal Chemistry Letters, 1996, 2031-2036, vol. 6, No. 16.
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Cram and Hammond, Organic Chemistry, 1964, 565-567, McGraw-Hill Book Co., New York, 2nd Edition.
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D. George et al., Antimicrobial Agents and Chemotherapy, pp. 86-91 ( Jan. 1996).

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