| 摘要 |
<p>A new process for the optical resolution of racemic mixtures of α-naphthyl-propionic acids of formula
<Chemistry id="chema01" num="0001"><Image id="ia01" he="30" wi="79" file="IMGA0001.TIF" imgContent="chem" imgFormat="TIFF" inline="no" /></Chemistry>This process comprises reacting a racemic mixture of a compound of formula
<Chemistry id="chema02" num="0002"><Image id="ia02" he="29" wi="81" file="IMGA0002.TIF" imgContent="chem" imgFormat="TIFF" inline="no" /></Chemistry>with an optically active substance of formula R<Sub>4</Sub>-NH<Sub>2</Sub> (III), said substance being a β-aminoalcohol, thus forming a pair of diastereoisomeric amides which are resolved into the single diastereoisomers by fractional crystallization. The obtained single diastereoisomeric amide is then hydrolized to give the desired optically active α-naphthyl-propionic acid of formula
<Chemistry id="chema03" num="0003"><Image id="ia03" he="29" wi="85" file="IMGA0003.TIF" imgContent="chem" imgFormat="TIFF" inline="no" /></Chemistry>In the above compound I → III and VI, R, is (C<Sub>1-6</Sub>)alkyl, R<Sub>2</Sub> stands for hydrogen, halogen, mercapto, (C<Sub>1-6</Sub>)alkylthio, phenylthio, benzylthio (C<Sub>1-6</Sub>)alkylsulfonyl, benzenesulfonyl, benzenesulfonyl substituted by halogen or (C<Sub>1-4</Sub>)alkyl, R<Sub>3</Sub> is a reactive group and R<Sub>4</Sub> is the residue of a primary or secondary alcohol.</p> |
