Patent ID: 6951948
Filing Date: 2005-10-04
Classification: C07D

Abstract:
1. A method of synthesizing highly substituted azole compounds having the general formula (Ia): wherein X is selected from the group consisting of NH, NR wherein is optionally substituted with one to three substituents independently selected from the group consisting of halogen, hydroxy, alkyl, halogenated alkyl; alkenyl, cycloalkyl, alkoxy, aryl, aralkyl, amino, mono- or di-substituted amino, cyano nitro, —COOR, —COR, —SO Z is —OR R R R is selected from the group consisting of alkyl, aryl, aralkyl, cycloalkyl, and fluorinated alkyl; wherein the aryl or aralkyl may be optionally substituted with one or more substituents independently selected from halogen, hydroxy, alkyl, halogenated alkyl, alkoxy, amino, mono- or di-substituted amino, cyano or nitro; R R which method comprises reacting a compound of formula (III) with a compound of formula (IV) wherein A is selected from F, Cl, Br or —OC(O)-t-butyl, and wherein V is a sterically hindered group, in a non-protic solvent; and then reacting with a compound of formula (V) wherein W is O, to form the corresponding compound of formula (Ic) and reacting the compound of formula (Ic) with a compound of formula (VI) to yield the corresponding compound of formula (Ia).