Method for preparing tert-leucine and analogues thereof in enantiomeric form and intermediates therein
    1.
    发明授权
    Method for preparing tert-leucine and analogues thereof in enantiomeric form and intermediates therein 失效
    以对映体形式制备叔 - 亮氨酸及其类似物的方法及其中间体

    公开(公告)号:US06180374B2

    公开(公告)日:2001-01-30

    申请号:US09131466

    申请日:1998-08-10

    IPC分类号: C07C26900

    摘要: Azlactone (3), or the opposite enantiomer thereof, undergoes biotransformation, using suitable enzymatic activity, in the presence of a compound YH to form a N-acyl-amino acid (2), wherein R1, R2 and R3 are each not hydrogen and are independently selected from groups containing up to 20 carbon atoms, optionally with any combination of R1, R2 and R3 being joined together to form at least one ring, X is selected from groups containing up to 20 carbon atoms, and Y is selected from the group consisting of —OH, -Oalkyl and -Nalkyl. Amino acid (1), or the opposite enantiomer thereof, can be prepared in high enantiomeric excess from N-acyl amino acid (2), by converting Y to OH.

    摘要翻译: 在化合物YH存在下,使用合适的酶活性,将吖内酯(3)或其相反对映异构体进行生物转化,形成N-酰基 - 氨基酸(2),其中R1,R2和R3各自不为氢, 独立地选自含有至多20个碳原子的基团,任选地与R 1,R 2和R 3的任何组合连接在一起形成至少一个环,X选自含有至多20个碳原子的基团,Y选自 由-OH,-O烷基和-N烷基组成的基团。 氨基酸(1)或其相反对映异构体可以通过将Y转化为OH,从N-酰基氨基酸(2)的高对映异构体过量制备。