OPTICAL RESOLUTION OF 3-BENZOYL-2-METHYLINDOLE DERIVATIVE

PURPOSE:To obtain the titled compound having optical activity easily, by reacting a (+ or -)-3-benzoyl-2-methylindole derivative with an optical active lactol to give an acetal derivative, subjecting it to optical resolution by a simple means, eliminating lactol from it. CONSTITUTION:A (+ or -)-3-be...

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Hauptverfasser: HASATO ATSUO, OKAMURA NORIAKI, TANAKA TOSHIO, SAKAUCHI KIYOSHI, YUU TAKESHI, KUROZUMI SEIJI, WATANABE KENZOU, OOBA TAKEO
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Sprache:eng
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Zusammenfassung:PURPOSE:To obtain the titled compound having optical activity easily, by reacting a (+ or -)-3-benzoyl-2-methylindole derivative with an optical active lactol to give an acetal derivative, subjecting it to optical resolution by a simple means, eliminating lactol from it. CONSTITUTION:A (+ or -)-3-benzoyl-2-methylindole derivative shown by the formula III (n is 1 or 2) is reacted with optical active lactol shown by the formulaIor formula II in the presence of an acid agent by dehydration method, to give an acetal derivative shown by the formula IV or formula V. A steroisomer of the acetal derivative is separated by chromatography, etc., the acetal bond is severed in the presence of acid agent, to give an optical active 3-benzoyl-2-methylindole derivative shown by the formula VI (* is asymmetric carbon atom) in high optical yield.