Patent ID: 6268510
Filing Date: 2001-07-31
Classification: C07D,Y02P

Abstract:
A process for the preparation of a compound of Formula I: ##STR25##wherein:R.sup.1 is: H, or halo;R.sup.2 is: C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 perfluoroalkyl, or phenyl;R.sup.3 is: H, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 cycloalkyl, CO.sub.2 Et, phenyl, unsubstituted or substituted with one, two, or three substituents selected from C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxyl, and nitro;R.sup.4, R.sup.5 and R.sup.6 are H, C.sub.1 -C.sub.6 alkyl, or phenyl, unsubstituted or substituted with one, two, or three R.sup.a substituents selected from: C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxyl, SO.sub.2 CH.sub.3 ;R.sup.4a is: H and R.sup.4b is H or C.sub.1 -C.sub.5 alkyl, when R.sup.4 is C.sub.1 -C.sub.6 alkyl, orR.sup.4a and R.sup.4b substitutents together represent a ring of seven carbons with alternating double bonds, that is unsubstituted or substituted with one, two, or three R.sup.a substituents selected from: C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxyl, SO.sub.2 CH.sub.3, when R.sup.4 represents a phenyl, as defined above in R.sup.4 ; andR.sup.7 is: --CO(CH.sub.3) or --CO(imidazolyl);which comprises the steps of:a) reacting a compound of Formula II ##STR26##with carbonyl diimidazole in an aprotic solvent, or with acetic anhydride in a solvent to produced a protected alcohol of Formula III: ##STR27##b) heating the protected alcohol of Formula III in the presence or absence of a solvent, at a temperature of about 0.degree. C. to about 100.degree. C. to produce the compound of Formula I, with the proviso that when R.sup.3 is cyclopropyl, R.sup.6 is phenyl and only one of R.sup.4 and R.sup.5 is H.