Patent ID: 6586594
Filing Date: 2003-07-01
Classification: A61P,C07D

Abstract:
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; R1 is C1-C6 alkyl; and â€œHetâ€  is pyrimidinyl optionally substituted by 1 to 3 substituents each independently selected from C1-C6 alkyl, C1-C4 alkoxy, halo, oxo, benzyl and benzyloxy, comprising (a) reacting 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 R1 and â€œHetâ€  are as previously defined for a compound of the formula (I) and X is chloro, bromo or iodo, said reaction (a) taking place in the presence of zinc; at least one of iodine or a Lewis acid; and an aprotic organic solvent: optionally further reacting the resulting compound of step (a) with an acid or base to form the corresponding acid addition or base salt thereof.