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    • 6. 发明授权
    • Process for preparation of oxyglutaric acid ester derivatives
    • 氧戊二酸酯衍生物的制备方法
    • US5717124A
    • 1998-02-10
    • US539173
    • 1995-10-04
    • Katsumasa HaradaAkio MatsushitaHiroshi SasakiYasuhiro Kawachi
    • Katsumasa HaradaAkio MatsushitaHiroshi SasakiYasuhiro Kawachi
    • C07F9/40C07F9/53C07F7/08
    • C07F9/4006C07F9/5304Y02P20/55
    • A process for preparing an oxyglutaric acid ester derivative of the formula: ##STR1## in which each of R.sup.1 and R.sup.2 is C.sub.1-5 alkoxy, C.sub.1-7 aralkyloxy, C.sub.7-9 halogenated aralkyloxy or phenyl, R.sup.4 is a hydroxyl-protecting group, and R.sup.5 is C.sub.1-10 alkyl which may have a substituent, comprises the steps of reacting a methyl phosphonate derivative or methyl phosphine oxide derivative with an oxyglutaric acid mono-ester to give a reaction product which comprises an oxyglutaric acid derivative having a phosphorus-containing group and a pentenedioic acid mono-ester (by-product), removing the pendenedioic acid mono-ester from the reaction product to isolate the oxyglutaric acid derivative, and converting the isolated oxyglutaric acid derivative into the oxyglutaric acid ester derivative. A process for obtaining an optically active oxyglutaric acid ester derivative is also disclosed.
    • 制备下式的其中R 1和R 2各自为C 1-5烷氧基,C 1-7芳烷氧基,C 7-9卤代芳烷基氧基或苯基的下式的下式的下列通式: R5是可以具有取代基的C1-10烷基,包括使甲基膦酸酯衍生物或甲基氧化膦衍生物与羟基戊二酸单酯反应,得到含有含磷的羟基戊二酸衍生物的反应产物 基和戊烯二酸单酯(副产物),从反应产物中除去邻苯二甲酸单酯以分离出氧戊二酸衍生物,并将分离的羟基戊二酸衍生物转化为羟基戊二酸酯衍生物。 还公开了获得光学活性的羟基戊二酸酯衍生物的方法。