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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