PHENYLGLYOXYLIC ACID DERIVATIVES AND THEIR PREPARATION AND USE

摘要

The invention provides novel phenylglyoxylic acid derivatives, which may be useful as intermediates for preparing stereoisomerically enriched drug compounds. The invention also provides methods of making phenylglyoxylic acid derivatives, and uses of phenylglyoxylic acid derivatives.

主权项

1. A method of making a phenylglyoxylic acid derivative comprising oxidizing a compound of Formula (II) wherein: R1 and R5 are hydrogen, halogen, C1-4 alkyl, C1-4 alkoxy, C1-4 haloalkyl, or C1-4 haloalkoxy; R3 is halogen, hydroxyl, cyano, C1-4 alkyl, C1-4 alkoxy, C1-4 haloalkyl, or C1-4 haloalkoxy; one of R2 and R4 is halogen, hydroxyl, cyano, C1-4 alkyl, C1-4 alkoxy, C1-4 haloalkyl, or C1-4 haloalkoxy, while the other is hydrogen, halogen, C1-4 alkyl, C1-4 alkoxy, C1-4 haloalkyl, or C1-4 haloalkoxy; R6, R7, R8, R9 are hydrogen, halogen, C1-4 alkyl, C1-4 alkoxy, C1-4 haloalkyl, or C1-4 haloalkoxy; R10 is hydrogen, C1-6 alkyl, or an alkali metal cation; and Z is C1-6 alkylene, which is optionally substituted one or more times by substitutents selected independently from the group consisting of halo, cyano, C1-4 haloalkyl, C1-4 haloalkoxy, phenyl, and oxo.