PYROGLUTAMATE SALT AND USE OF THE SAME IN OPTICAL RESOLUTION OF INTERMEDIATE FOR SYNTHESIS OF DEXTROCETIRIZINE AND LEVOCETIRIZINE

PROBLEM TO BE SOLVED: To provide a simpler preparation method for an enantiomerically and essentially pure compound like levocetirizine or the like by using a novel and enantiomerically and essentially pure intermediate.SOLUTION: There is provided a (S)-2-[4-(4-chlorobenzhydryl)piperazine-1-yl]-etho...

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Hauptverfasser: ATES CELAL, PALACIO MAGALI
Format: Patent
Sprache:eng
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Zusammenfassung:PROBLEM TO BE SOLVED: To provide a simpler preparation method for an enantiomerically and essentially pure compound like levocetirizine or the like by using a novel and enantiomerically and essentially pure intermediate.SOLUTION: There is provided a (S)-2-[4-(4-chlorobenzhydryl)piperazine-1-yl]-ethoxyacetamide-(S)-pyrrolidone-5-carboxylic acid salt, (R)-2-[4-(4-chlorobenzhydryl)piperazine-1-yl]-ethoxyacetamide-(S)-pyrrolidone-5-carboxylic acid salt, (S)-2-[4-(4-chlorobenzhydryl)piperazine-1-yl]-ethoxyacetamide-(R)-pyrrolidone-5-carboxylic acid salt, or (R)-2-[4-(4-chlorobenzhydryl)piperazine-1-yl]-ethoxyacetamide-(R)-pyrrolidone-5-carboxylic acid salt. There is also provided the preparation method for (S)-2-[4-(4-chlorobenzhydryl)piperazine-1-yl]-ethoxyacetamide (I) and (R)-2-[4-(4-chlorobenzhydryl)piperazine-1-yl]-ethoxyacetamide (II) by chemical resolution of a mixture.