Method for preparing 2-thienylethylamine derivatives
    3.
    发明授权
    Method for preparing 2-thienylethylamine derivatives 有权
    2-噻吩乙胺衍生物的制备方法

    公开(公告)号:US6080875A

    公开(公告)日:2000-06-27

    申请号:US380450

    申请日:1999-09-02

    CPC分类号: C07D333/20

    摘要: The present invention relates to a process for the preparation of 2-thienylethylamine derivatives of general formula: ##STR1## as well as their acid addition salts, in which R represents a halogen atom and R.sub.1 represents a C.sub.1 -C.sub.4 alkyl group, characterized in that a thienylglycidic derivative of general formula: ##STR2## in which M represents an alkali metal atom or a fraction of an alkaline-earth metal atom, is reacted with a phenylglycine ester, optionally in the form of a strong acid salt, of general formula: ##STR3## in which R and R.sub.1 have the same meaning as above, in the presence of an alkali metal borchydride of general formula:X--Y IVin which X represents an alkali metal atom and Y represents a group of formula:--BH.sub.3 CN or --BH.sub.(4-w) Z.sub.win which Z represents a carboxylic acid residue and optionally in the presence of a C.sub.1 -C.sub.4 carboxylic acid, which gives the desired compound in the form of a free base which can be treated, if necessary, with an acid in order to obtain an addition salt of this compound.

    摘要翻译: PCT No.PCT / FR98 / 00441 Sec。 371 1999年9月2日第 102(e)1999年9月2日PCT 1998年3月5日PCT PCT。 第WO98 / 39322号公报 日本公开日1998年9月11日本发明涉及制备通式的2-噻吩乙胺衍生物及其酸加成盐的方法,其中R表示卤素原子,R1表示C1-C4烷基,其特征在于 其中通式为:其中M表示碱金属原子或碱土金属原子的部分的噻吩基缩水甘油衍生物与任选呈强酸盐形式的苯基甘氨酸酯反应,通式为:在 其中R和R 1具有与上述相同的含义,在通式为X-YIV的碱金属硼氢化物的存在下,其中X代表碱金属原子,Y代表下列基团:-BH 3 CN或-BH(4- w)Zw,其中Z表示羧酸残基并且任选地在C1-C4羧酸存在下,其得到游离碱形式的所需化合物,如果需要,可以用酸处理,以便 获得此加成盐 复合。

    Process for the preparation of a free L .alpha.-amino acid
    5.
    发明授权
    Process for the preparation of a free L .alpha.-amino acid 失效
    制备游离Lα-氨基酸的方法

    公开(公告)号:US4540792A

    公开(公告)日:1985-09-10

    申请号:US472479

    申请日:1983-03-07

    CPC分类号: C12P41/005 C07D213/48

    摘要: This invention relates to a process for the preparation of free L .alpha.-amino acids by the complete conversion of their D antipodes taken individually or possibly in racemic mixtures.The process according to the present invention is characterized in that the D antipodes of an ester of said .alpha.-amino acid is racemized in the presence of a chemical catalyst formed by at least one aromatic aldehyde corresponding to the general formula: ##STR1## wherein: Ar represents an aromatic ring optionally containing a heteroatom, such as nitrogen, andB represents a basic function,to produce a mixture in dynamic equilibrium of the two forms D and L of said ester, the ester which is present in the L form is hydrolyzed enzymatically and irreversibly to produce the corresponding stereostable L .alpha.-amino acid, said stages of chemical racemization and of enzymatic hydrolysis being carried out under identical reaction conditions, and the free L .alpha.-amino acid is recovered.

    摘要翻译: 本发明涉及一种通过其单独或可能在外消旋混合物中完全转化其对映体的方法制备游离的L-α-氨基酸的方法。 根据本发明的方法的特征在于,所述α-氨基酸的酯的D对映体在由至少一种芳族醛形成的化学催化剂的存在下外消旋化,所述芳族醛对应于以下通式: )其中:Ar表示任选地含有杂原子如氮的芳环,B表示碱性官能团,以产生所述酯的两种形式D和L的动态平衡混合物,所述酯存在于L 形式水解并不可逆地产生相应的立体立构的Lα-氨基酸,在相同的反应条件下进行化学外消旋和酶水解的所述阶段,回收游离的Lα-氨基酸。