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    • 1. 发明授权
    • Method for producing optically active 1-phenylethylamines
    • 光学活性1-苯基乙胺的制备方法
    • US6034278A
    • 2000-03-07
    • US194719
    • 1998-12-17
    • Walter MerzMartin LittmannUdo KraatzChristoph Mannheims
    • Walter MerzMartin LittmannUdo KraatzChristoph Mannheims
    • C07B53/00C07C209/88C07C211/27C07C211/29C07C209/00
    • C07C209/88
    • The invention concerns a new method for producing optically active 1-phenylethylamines, wherein (a) racemic 1-phenylethylamines are reacted with (S)-(-)-N-phenylcarbamate lactic acid in the presence of an aliphatic or aromatic hydrocarbon and in the presence of a lower aliphatic alcohol, wherein the reaction components are measured so that for every mole of racemic amine, between 0.25 and 0.5 mole of (S)-(-)-N-phenylcarbamate lactic acid are present, the reaction mixture is then concentrated at a liquid-phase temperature of up to 40.degree. C., the resulting solid product is separated, treated with diluted, aqueous alkaline lye in the presence of a hydrocarbon, and the respective (R)-amine is isolated by distillation from the organic phase, and if necessary, (b) the mother liquor remaining after the separation of the solid product is reacted in the presence of a lower aliphatic alcohol with (S)-(-)-N-phenylcarbamate lactic acid, wherein the reaction components are measured so that the molar quantity of (S)-(-)-N-phenylcarbamate lactic acid is twice as great as the quantity of (R)-amine still remaining in the mother liquor, the reaction mixture is then concentrated at a liquid-phase temperature of up to 40.degree. C., the resulting solid product is separated and the (S)-amine is isolated by distillation from the mother liquor.
    • PCT No.PCT / EP97 / 02988第 371日期1998年12月17日第 102(e)日期1998年12月17日PCT提交1997年6月9日PCT公布。 公开号WO97 / 49665 PCT 日期1997年12月31日本发明涉及一种用于制备光学活性1-苯基乙胺的新方法,其中(a)外消旋1-苯乙基胺与(S) - ( - ) - N-苯基氨基甲酸酯乳酸在脂肪族或 芳族烃和低级脂族醇的存在下,其中测量反应组分,使得对于每摩尔外消旋胺,存在0.25至0.5摩尔(S) - ( - ) - N-苯基氨基甲酸酯乳酸, 然后将反应混合物在高达40℃的液相温度下浓缩,分离得到的固体产物,在烃存在下用稀释的碱性碱水溶液处理,分离出(R) - 胺 (b)将固体产物分离后剩余的母液在低级脂族醇与(S) - ( - ) - N-苯基氨基甲酸酯乳酸的存在下反应, 其中测量反应组分 d,使得(S) - ( - ) - N-苯基氨基甲酸酯乳酸的摩尔量是母液中残留的(R) - 胺的量的两倍,然后将反应混合物以液 - 相温度高达40℃,分离得到的固体产物,并通过蒸馏从母液中分离出(S) - 胺。