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    • 88. 发明授权
    • Process for producing N-acylphenylalanines
    • N-酰基苯丙氨酸的制备方法
    • US4612388A
    • 1986-09-16
    • US719300
    • 1985-04-03
    • Ryuichi MitaToshio KatohChojiro HiguchiAkihiro Yamaguchi
    • Ryuichi MitaToshio KatohChojiro HiguchiAkihiro Yamaguchi
    • C07C231/10C07C67/00C07C231/00C07C231/12C07C233/46C07C233/47C07C233/82C07C233/83C07C99/06
    • C07C233/46
    • 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.
    • 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 。