发明名称 Preparation of triazoles by organometallic addition to ketones and intermediates therefor
摘要 The invention provides a process for the preparation of a compound of the formula: or an acid addition or base salt thereof, wherein R is phenyl optionally substituted by 1 to 3 substituents each independently selected from halo and trifluoromethyl; R<SUP>1 </SUP>is C<SUB>1</SUB>-C<SUB>6 </SUB>alkyl; and "Het" is pyrimidinyl optionally substituted by 1 to 3 substituents each independently selected from C<SUB>1</SUB>-C<SUB>4 </SUB>alkyl, C<SUB>1</SUB>-C<SUB>4 </SUB>alkoxy, 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 R<SUP>1 </SUP>and "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.
申请公布号 US7193083(B2) 申请公布日期 2007.03.20
申请号 US20050120739 申请日期 2005.05.02
申请人 PFIZER, INC. 发明人 BUTTERS MICHAEL;PETTMAN ALAN JOHN
分类号 C07D403/10;A61K31/506 主分类号 C07D403/10
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