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    • 14. 发明授权
    • Racemization process for an optically active carboxylic acid or ester
thereof
    • 光学活性羧酸或其酯的外消旋化方法
    • US5221765A
    • 1993-06-22
    • US825150
    • 1992-01-24
    • Deepak R. PatilAzfar A. ChoudhuryAbbas Kadkhodayan
    • Deepak R. PatilAzfar A. ChoudhuryAbbas Kadkhodayan
    • B01J31/02C07B55/00C07B61/00C07C51/487C07C57/30C07C69/612
    • C07C51/487C07B55/00
    • A method for racemizing an optically active carboxylic acid, or ester thereof, of the formula: ##STR1## where R.sub.1 is hydrogen or C.sub.1 to C.sub.6 linear or branched alkyl; R.sub.2, R.sub.3 and R.sub.4 are different and are hydrogen or C.sub.1 to C.sub.6 linear or branched alkyl, C.sub.1 to C.sub.6 linear or branched haloalkyl, aralkyl, cycloalkyl, alkyl substituted cycloalkyl, C.sub.6 to C.sub.10 aryl, C.sub.1 to C.sub.6 linear or branched alkoxy, C.sub.6 to C.sub.10 aryloxy, C.sub.1 to C.sub.6 alkylthio, C.sub.2 to C.sub.8 cycloalkylthio, C.sub.6 to C.sub.10 arylthio, C.sub.6 to C.sub.10 arylcarbonyl, C.sub.4 to C.sub.8 cycloalkenyl, trifluoromethyl, halo, C.sub.4 to C.sub.5 heteroaryl, C.sub.10 to C.sub.14 aryl, or biphenyl unsubstituted or substituted with methyl or halo, comprising heating said optically active carboxylic acid or ester thereof in the presence of water at a temperature of from about 75.degree. C. to about 200.degree. C. in the presence of a catalytically effective amount of an aliphatic, aromatic or mixed aliphatic and aromatic tertiary amine for a time sufficient to racemize said carboxylic acid or ester thereof.
    • 其中R 1为氢或C 1至C 6直链或支链烷基的式I的光学活性羧酸或其酯的外消旋化方法: R2,R3和R4不同,为氢或C1至C6直链或支链烷基,C1至C6直链或支链卤代烷基,芳烷基,环烷基,烷基取代的环烷基,C6至C10芳基,C1至C6直链或支链烷氧基,C6至 C10芳氧基,C1至C6烷硫基,C2至C8环烷硫基,C6至C10芳硫基,C6至C10芳基羰基,C4至C8环烯基,三氟甲基,卤素,C4至C5杂芳基,C10至C14芳基或未取代或被甲基或 卤素,包括在水存在下,在约75℃至约200℃的温度下,在催化有效量的脂族,芳族或混合脂族的存在下加热所述光学活性羧酸或其酯,和 芳族叔胺足以使所述羧酸或其酯外消旋的时间。