Patent ID: 6294560
Filing Date: 2001-09-25
Classification: A61P,C07B,C07C,C07D

Abstract:
A process for forming a substituted oxazoline compound of Formula II: ##STR43##said method comprising:(a) deprotonating a substituted aryl or heteroaryl oxazoline of Formula I: ##STR44##by treating said substituted aryl or heteroaryl oxazoline with a strong base to form an enolate; and(b) transmetallating said enolate with a metal selected from the group consisting of titanium, aluminum tin, zinc, magnesium and boron, and thereafter reacting with a formyl amide of Formula XIV: ##STR45##wherein for each of Formulae I, II and XIV:R.sup.1 is alkyl, alkenyl, alkynyl, cycloalkyl, aryl, alkaryl, aralkyl, where the ring portion of any of said aryl, aralkyl, or alkaryl can be optionally substituted;R.sup.2 is alkyl, cycloalkyl, aryl, alkaryl, aralkyl, alkoxy, hydroxy, alkoxyalkyl, or amido, where the ring portion of any of said aryl, aralkyl, or alkaryl can be optionally substituted;R.sup.3 is alkyl, alkenyl, alkynyl, cycloalkyl, aryl, alkaryl, any of which can be optionally substituted;R.sup.4 is optionally substituted aryl or optionally substituted heteroaryl; andR.sup.5 and R.sup.6 are independently one of alkyl or alkaryl; or R.sup.5 and R.sup.6 when taken together with the nitrogen atom to which they are attached form a 5- to 7-membered heterocyclic ring, which can be optionally substituted, and which optionally include an additional oxygen or nitrogen atom.