Importance

Loading Importance Indicators...

Abstract

This invention relates to processes for the synthesis of various optically active amino pyrrolidinyl stereoisomers, or enantiomers, that may be attached to quinolonecarboxylic acids or naphthyridones. Processes and essential intermediates are disclosed and claimed for the synthesis of compounds represented by the structure shown in FIG. BG.sub.4-1, where R.sup.50, R.sup.6 and R.sup.9 are defined independently and are H, -(C.sub.1 -C.sub.8)alkyl, -(C.sub.3 -C.sub.8)cycloalkyl, -(C.sub.1 -C.sub.8)alkyl-(C.sub.3 -C.sub.8)cycloalkyl, -(C.sub.6 -C.sub.12 aryl), -(C.sub.1 -C.sub.8)alkyl-(C.sub.6 -C.sub.12 aryl), or the aryl or alkyl is substituted with one to three of the following groups, (C.sub.6 -C.sub.12 aryl), (C.sub.1 -C.sub.3)alkyl, (C.sub.1 -C.sub.3)alkoxy, halogen, trifluoromethyl; where R.sup.2 is -(C.sub.1 -C.sub.8)alkyl, -(C.sub.3 -C.sub.8)cycloalkyl, -(C.sub.1 -C.sub.8)alkyl-(C.sub.3 -C.sub.8)cycloalkyl, -(C.sub.6 -C.sub.12 aryl), -(C.sub.1 -C.sub.8)alkyl-(C.sub.6 -C.sub.12 aryl), or the aryl or alkyl is substituted with one to three of the following groups, -(C.sub.6 -C.sub.12 aryl), -(C.sub.1 -C.sub.3)alkyl,-(C.sub.1 -C.sub.3)alkoxy, halogen, trifluoromethyl; depending upon the starting materials used, compounds represented by the structure shown by FIG. BG.sub.4-1 may have one of either of the two stereochemical arrangements shown, or, if the starting materials are a racemic mixture, the reaction may produce a 1:1 ratio of the combination of products shown in FIG. BG.sub.4-1, i.e. a racemic mixture.

Loading the Abstract Image...

First Claim