Patent ID: 6245914
Filing Date: 2001-06-12
Classification: A61P,C07D,C07F

Abstract:
A process for the formation of a compound of the formula (I): ##STR25##or a pharmaceutically acceptable salt form thereof; wherein:R.sup.1 is selected from H or NHR.sup.1a ;R.sup.1a is --C(.dbd.O)--O--R.sup.1b ;R.sup.1c is H;R.sup.2 is H;R.sup.3 and R.sup.4 are H;n is 1;a is a single bond;said process comprising:contacting a compound of formula (VI): ##STR26##wherein:Z is selected from R.sup.6 SO.sub.2 -- or (R.sup.7).sub.3 Si--;R.sup.6 is selected from the group consisting of H, CF.sub.3, CF.sub.2 CF.sub.3, CF.sub.2 CF.sub.2 CF.sub.3, CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3, C.sub.1 -C.sub.8 alkyl, C.sub.1 -C.sub.8 perfluoroalkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl, C.sub.3 -C.sub.11 cycloalkyl, C.sub.4 -C.sub.11 cycloalkylalkyl, aryl(C.sub.1 -C.sub.6 alkyl)-, C.sub.1 -C.sub.6 alkoxy, C.sub.7 -C.sub.10 arylalkyloxy, aryloxy and aryl substituted with 0-5 R.sup.6c ;R.sup.6c is selected from the group consisting of H, halo, CF.sub.3, CN, NO.sub.2, NR.sup.6d R.sup.6e, C.sub.1 -C.sub.8 alkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.3 -C.sub.11 cycloalkyl, C.sub.4 -C.sub.11 cycloalkylalkyl, aryl, aryl(C.sub.1 -C.sub.6 alkyl)-, C.sub.1 -C.sub.6 alkoxy, and C.sub.2 -C.sub.5 alkoxycarbonyl;R.sup.6d and R.sup.6e are independently selected from the group consisting of H, C.sub.1 -C.sub.10 alkyl, C.sub.2 -C.sub.10 alkoxycarbonyl, C.sub.2 -C.sub.10 alkylcarbonyl, C.sub.1 -C.sub.10 alkylsulfonyl, aryl, aryl(C.sub.1 -C.sub.10 alkyl)sulfonyl, arylsulfonyl, heteroaryl(C.sub.1 -C.sub.4 alkyl)sulfonyl, heteroarylcarbonyl, heteroarylsulfonyl, or heteroarylalkylcarbonyl, wherein said aryl and heteroaryl are optionally substituted with 0-3 substituents selected from the group consisting of C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, halo, CF.sub.3, and NO.sub.2 ;R.sup.7 is selected independently from C.sub.1 -C.sub.10 alkyl or aryl substituted 0-3 R.sup.7a ; andR.sup.7a is C.sub.1 -C.sub.10 alkyl;with hydrogen under a suitable pressure in the presence of a hydrogenation catalyst to form a compound of formula (I) or a pharmaceutically acceptable salt form thereof.