| 摘要 |
A method for preparing optically active benzoxazine derivatives is provided to reduce the preparation procedure and improve preparation yield by forming a salt and recrystallizing the salt instead of using amide synthesis method. The method for preparing optically active benzoxazine derivatives represented by the formula(1) comprises the steps of: (a) reacting benzoxazine compounds represented by the formula(2) with chiral organic acid to prepare chiral organic acid salt of benzoxazine compounds represented by the formula(3); and (b) separating an optical isomer from the chiral organic acid salt of benzoxazine compounds represented by the formula(3) by recrystallization method with a mixed organic solvent, wherein R is C1-C4 linear or branched alkyl group; OA is L-tartaric acid, L-mandelic acid or L-methylphenylpropionic acid for forming salts; the step(a) is performed in the mixed organic solvent of acetone and ethanol; and the mixed organic solvent in step(b) contains dichloromethane and sodium carbonate solution.
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