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    Process for producing N-acylphenylalanines
    8.
    发明授权
    Process for producing N-acylphenylalanines 失效
    N-酰基苯丙氨酸的制备方法

    公开(公告)号：US4612388A

    公开(公告)日：1986-09-16

    申请号：US719300

    申请日：1985-04-03

    申请人： Ryuichi Mita ,  Toshio Katoh ,  Chojiro Higuchi ,  Akihiro Yamaguchi

    发明人： Ryuichi Mita ,  Toshio Katoh ,  Chojiro Higuchi ,  Akihiro Yamaguchi

    IPC分类号： C07C231/10 ,  C07C67/00 ,  C07C231/00 ,  C07C231/12 ,  C07C233/46 ,  C07C233/47 ,  C07C233/82 ,  C07C233/83 ,  C07C99/06

    CPC分类号： C07C233/46

    摘要： Disclosed herein is a process for producing an N-acyl-substituted or unsubstituted phenylalanine comprising hydrolyzing a 2-substituted-4-substituted or unsubstituted benzylidene-5-oxazolone with alkali, adjusting pH of the reaction solution containing its hydrolysis product with acid at 5-9 and reducing the resultant reaction solution catalytically in the presence of a palladium or platinum reducing catalyst.In accordance with the process of the present invention, time duration required for effecting the reduction can be shortened markedly in comparison with the reduction in an aqueous strong alkaline solution. Moreover, the catalyst recovered after completion of the reduction can be used repeatedly without any additional treatment and without any observed lowering in its activity. Accordingly, the reduction using the recovered catalyst may proceed in practically the same time as in the case of using a fresh catalyst.In the process of the present invention, the reduction is carried out continuously without isolating the alkaline hydrolysis product, i.e., a substituted or unsubstituted N-acylaminocinnamic acid from the reaction mixture, so that the process is featured advantageously by simplified process and improved overall yield.

    摘要翻译： 本文公开了N-酰基取代或未取代的苯丙氨酸的制备方法，其包括用碱水解2-取代-4-取代或未取代的亚苄基-5-恶唑酮，调节含有其水解产物的反应溶液的pH为5 -9并在钯或铂还原催化剂的存在下催化还原所得的反应溶液。 根据本发明的方法，与强碱性水溶液的降低相比，可以显着缩短实现还原所需的时间。 此外，还原后还原反应的催化剂可以重复使用，无需任何额外的处理，并且没有观察到其活性降低。 因此，使用回收的催化剂的还原可以与使用新鲜催化剂的情况几乎相同的时间进行。 在本发明的方法中，还原是从反应混合物中分离碱性水解产物，即取代或未取代的N-酰氨基肉桂酸，连续进行，使得该方法有利地通过简化的方法和改进的总产率 。

    Preparation process of .alpha.-l-aspartyl-l-phenyl-alanine methyl ester or hydrohalide thereof
    10.
    发明授权
    Preparation process of .alpha.-l-aspartyl-l-phenyl-alanine methyl ester or hydrohalide thereof 失效
    α-1-天冬氨酰基-1-苯基 - 丙氨酸甲酯或其氢卤化物的制备方法

    公开(公告)号：US4918216A

    公开(公告)日：1990-04-17

    申请号：US357618

    申请日：1989-05-25

    申请人： Ryuichi Mita ,  Toshio Katoh ,  Chojiro Higuchi ,  Takeshi Oura ,  Akihiro Yamaguchi

    发明人： Ryuichi Mita ,  Toshio Katoh ,  Chojiro Higuchi ,  Takeshi Oura ,  Akihiro Yamaguchi

    IPC分类号： A23L27/30 ,  C07K1/02 ,  C07K5/06 ,  C07K5/075

    CPC分类号： C07K5/0613

    摘要： .alpha.-L-aspartyl-L-phenylalanine methyl ester or the hydrohalide thereof is prepared by esterifying .alpha.-L-aspartyl-L-phenylalanine or .alpha.-L-aspartyl-L-phenylalanine which has been formed in situ by treating an N-protected-.alpha.-L-aspartyl-L-phenylalanine in an aqueous solution of sulfuric acid or a methanol-containing aqueous solution of sulfuric acid in the presence of an alkali metal halide or alkaline earth metal halide in a medium composed of sulfuric acid, water and methanol, thereby to allow the resulting .alpha.-L-aspartyl-L-phenyl-alanine methyl ester to precipitate as its corresponding hydrohalide, and then isolating the hydrohalide; and when the preparation of the methyl ester is desired, neutralizing the hydrohalide.

    摘要翻译： α-L-天冬氨酰基-L-苯丙氨酸甲酯或其氢卤化物通过酯化通过将N-保护的N-保护基团经过N-保护基团处理而形成的α-L-天冬氨酰基-L-苯丙氨酸或α-L-天冬氨酰基-L-苯丙氨酸 α-L-天冬氨酰基-L-苯丙氨酸在硫酸水溶液或含甲醇的硫酸水溶液中，在碱金属卤化物或碱土金属卤化物存在下，在由硫酸，水和 从而使所得的α-L-天冬氨酰-L-苯基 - 丙氨酸甲酯作为其对应的氢卤酸盐沉淀，然后分离氢卤化物; 并且当需要制备甲酯时，中和氢卤化物。