Optically active 1-phenyl-2-substituted propane derivatives and methods of producing the same
    3.
    发明授权
    Optically active 1-phenyl-2-substituted propane derivatives and methods of producing the same 失效
    光学活性的1-苯基-2-取代的丙烷衍生物及其制备方法

    公开(公告)号:US06248573B1

    公开(公告)日:2001-06-19

    申请号:US09208842

    申请日:1998-12-10

    IPC分类号: C12P722

    摘要: An (S)-1-phenyl-2-substituted propane derivative shown by the following formula (I) wherein R1 and R2 represent a lower alkyl group, etc., or R1 and R2 may form together an alkylene group, etc.; R3, R4 and R5 represent a hydrogen atom, etc.; and X represents a hydroxyl group which may be protected with a protective group, or a halogen atom etc., can readily be produced (i) by permitting a microorganism belonging to the genus Torulaspora, the genus Candida, the genus Pichia or the like to act on a phenylacetone derivative and asymmetrically reducing the compound, or (ii) by sterically inverting an (R)-enantiomer. (R,R)-1-phenyl-2-[(2-phenyl-1-methylethyl)amino]ethanol derivative having a high optical purity can easily be obtained from the compound of the formula (I). The ethanol derivative is useful as an anti-obesity agent and the like.

    摘要翻译: 式(I)所示的(S)-1-苯基-2-取代的丙烷衍生物,其中R1和R2表示低级烷基等,或者R1和R2可以一起形成亚烷基等; R3,R4和R5代表氢原子等; X表示可以被保护基或卤素原子等保护的羟基,可容易地制备(i)通过使属于弧菌属,假丝酵母​​属,毕赤酵母属等的微生物, 作用于苯基丙酮衍生物并不对称地还原化合物,或(ii)通过空间反转(R) - 对映异构体。 (I)化合物可以容易地获得具有高光学纯度的(R,R)-1-苯基-2 - [(2-苯基-1-甲基乙基)氨基]乙醇衍生物。 乙醇衍生物可用作抗肥胖剂等。

    Process for preparing N-substituted amino acid esters
    7.
    发明授权
    Process for preparing N-substituted amino acid esters 失效
    制备N-取代氨基酸酯的方法

    公开(公告)号:US5055588A

    公开(公告)日:1991-10-08

    申请号:US520961

    申请日:1990-05-09

    IPC分类号: C07C227/08

    CPC分类号: C07C227/08

    摘要: A process for preparing N-substituted amino acid esters having the formula (I): ##STR1## wherein R.sub.1 and R.sub.4, the same or different, are an alkyl, aralkyl, cycloalkyl or aryl group; and R.sub.2 and R.sub.3, the same or different,are an alkyl, aralkyl, aryl, heterocycle-alkyl, aminoalkyl or guanidylalkyl, by the reaction of .alpha.-amino acid esters with .alpha.-substituted carboxylic acid esters, under the condition of substantially free from solvent, which can afford their optical isomers in a good yield.

    摘要翻译: 制备具有式(I)的N-取代氨基酸酯的方法:其中R 1和R 4相同或不同,为烷基,芳烷基,环烷基或芳基; 并且R 2和R 3相同或不同,是烷基,芳烷基,芳基,杂环烷基,氨基烷基或胍基烷基,通过α-氨基酸酯与α-取代的羧酸酯的反应,在基本上不含 溶剂,其可以以良好的产率提供它们的旋光异构体。