Patent ID: 6040442
Filing Date: 2000-03-21
Classification: A61P,C07D

Abstract:
A process for preparing a compound of formula 1 ##STR20## wherein R.sup.1 is hydrogen, halogen, NR.sup.6 R.sup.7, R.sup.4, --OR.sup.4, --SR.sup.4, SOR.sup.4, --SO.sub.2 R.sup.4, C.sub.3-10 -cycloalkyl, C.sub.4-12 -(cycloalkylalkyl), --Z--C.sub.3-10 -cycloalkyl, --Z--C.sub.4-12 -(cycloalkylalkyl), --OR.sup.5 Y, --SR.sup.5 Y, --OR.sup.5 ZY, --SR.sup.5 ZY, --OR.sup.5 ZR.sup.4, --SR.sup.5 ZR.sup.4, phenyl or benzyloxycarbonyl, or phenyl or benzyloxycarbonyl substituted with one or more substituents independently selected from halogen, --CN, C.sub.1-4 -alkyl, C.sub.1-4 -alkoxy, --OCF.sub.3, or --CF.sub.3 ;R.sup.4 is C.sub.1-15 -alkyl, C.sub.2-15 -alkenyl, or C.sub.2-15 -alkynyl, each of which is optionally substituted with one or more substituents independently selected from halo, --CF.sub.3, --CN, Y, phenyl or phenoxy, or phenyl or phenoxy substituted with one or more substituents independently selected from halo, --CN, C.sub.1-4 -alkyl, C.sub.1-4 -alkoxy, --OCF.sub.3, or --CF.sub.3 ;Z is oxygen or sulphur;R.sup.5 is C.sub.1-15 -alkylene, C.sub.2-15 -alkenylene, or C.sub.2-15 -alkynylene;Y is a 5 or 6 membered heterocyclic group;R.sup.6 and R.sup.7 independently are C.sub.1-6 -alkyl; orR.sup.6 and R.sup.7 together with the nitrogen atom from a 4- to 6-membered ring;G is an azacyclic or azabicyclic ring system selected from: ##STR21## R.sup.1 and R.sup.2, independently, are hydrogen, C.sub.1-15 -alkyl, C.sub.2-5 -alkenyl, C.sub.2-5 -alkynyl, C.sub.1-10 -alkoxy, or C.sub.1-5 -alkyl substituted with one or more substituents independently selected from --COR.sup.6', halo or phenyl;R.sup.6' is hydrogen or C.sub.1 -C.sub.3 alkyl;R.sup.3 is C.sub.1-5 -alkyl, C.sub.2-5 -alkenyl or C.sub.2-5 -alkynyl;m, n, p and p, independently, are 0, 1 or 2;q is 1 or 2; and- - - is a single or double bond;comprising contacting a compound of formula 2 ##STR22## wherein R' is as defined supra; with a compound of the formula G--OH, a phosphorous(III) compound, and a diester of azodicarboxylate.