逆相分配系高速液体クロマトグラフィーによるカルボキシル基含有医薬品の光学分割を目的としたキラル誘導体化

概要

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We investigated diastereoisomer derivatization procedures of carboxylic drugs by the mixed anhydride (MA) method, phosphate ester activation method and DCC coupling method using reversed phase HPLC. As a result, the MA method was found to be suitable as a derivatization method in terms of sample handling, rapidity and practical use. We applied the MA method to the derivatization of phenyl acetate drugs, such as ketoprofen, to L-leucinamide diastereoisomer or R-naphthylethyl amine diastereoisomer. Good stereo isomeric resolutions of L-leucinamide diastereoisomers were obtained by reversed phase HPLC. These results suggest that derivatization to L-leucinamide diastereoisomers by the MA method is suitable for chiral separation of carboxylic drugs using reversed phase HPLC.
社団法人日本分析化学会の論文
1994-12-05