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    • 52. 发明公开
    • Process for producing N-acylphenylalanines
    • Verfahren zur Herstellung von N-酰基苯丙氨酸。
    • EP0161796A1
    • 1985-11-21
    • EP85302503.9
    • 1985-04-09
    • MITSUI TOATSU CHEMICALS, Inc.
    • Mita, RyuichiKatoh, ToshioHiguchi, ChojiroYamaguchi, Akihiro
    • C07C103/48C07B57/00C07K5/02
    • C07C233/46
    • An N-acyl-substituted or unsubstituted phenylalanine is prepared by hydrolyzing a 2-substituted-4-substituted or unsubstituted benzylidene-5-oxazolone with an alkali, adjusting the reaction system containing its hydrolysis product with acid to a pH of 5 - 9 and reducing the resultant reaction solution catalytically in the presence of a palladium or platinum reducing catalyst. The reduction is carried out continuously without isolating the alkaline hydrolysis product, i.e., a substituted or unsubstituted N-acylaminocinnamic acid from the reaction system.
      The catalyst can be recovered after completion of the reduction and used repeatedly without additional treatment and without any observed lowering in its catalytic activity. Accordingly, the reductions using the recovered catalyst may proceed at pratically the same rate as reductions using a fresh catalyst.
    • N-酰基取代或未取代的苯丙氨酸通过用碱水解2-取代-4-取代或未取代的亚苄基-5-恶唑酮来制备,将含有其水解产物的反应体系用酸调节至pH为5-9, 在钯或铂还原催化剂存在下催化还原所得反应溶液。 在不从反应体系中分离碱性水解产物即取代或未取代的N-酰氨基肉毒酸的情况下,进行还原。 在完成还原后可以回收催化剂,反复使用,无需额外的处理,并且没有观察到其催化活性降低。 因此,使用回收的催化剂的减少量可以以与使用新鲜催化剂的还原率相同的速率进行。