Convenient synthesis of antisepsis agent TAK-242 by novel optical resolution through diastereomeric N-acylated sulfonamide derivative |
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| Authors: | Atsuko Nishiguchi Tomomi Ikemoto Kiminori Tomimatsu |
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| Affiliation: | Chemical Development Laboratories, Takeda Pharmaceutical Company Limited, 2-17-85 Jusohonmachi, Yodogawa-ku, Osaka 532-8686, Japan |
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| Abstract: | A convenient synthesis method of antisepsis agent TAK-242 ((R)-1) through diastereomeric resolution was developed. By condensation of racemate rac-1 with chiral acid (S)-O-acetylmanderic acid (6a), the desired diastereomer 5a was isolated with 98% de in 39% yield by simple crystallization. Deacylation of 5a with aq NaOH followed by recrystallization provided (R)-1 with 99% ee in 20% yield from rac-1. |
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| Keywords: | Antisepsis agent Diastereomeric resolution Sulfonamide Chiral acid Deacylation |
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