Process for producing optically active cyanohydrins
    3.
    发明授权
    Process for producing optically active cyanohydrins 失效
    光学活性氰醇的制备方法

    公开(公告)号:US5900503A

    公开(公告)日:1999-05-04

    申请号:US68605

    申请日:1998-05-11

    摘要: An optically active cyanohydrin represented by the following general formula (1): ##STR1## wherein each of R1 and R2 is a hydrogen atom or an amino-protecting group, and the configurations relating to the carbon atoms at the *2-position and *3-position are as follows: in the case of the carbon atom at the *2-position being in R-configuration, the carbon atom at the *3-position is in S-configuration, and in the case of the carbon atom at the *2-position being in S-configuration, the carbon atom at the *3-position is in R-configuration, can be efficiently produced by crystallizing one of the optically active cyanohydrins while treating a mixture of cyanohydrin diastereomers in the presence of an amine and an organic solvent to change the configuration relating to the carbon atom at the 2-position and thereby cause isomerization.

    摘要翻译: PCT No.PCT / JP97 / 00319 Sec。 371日期:1998年5月11日 102(e)日期1998年5月11日PCT提交1997年2月7日PCT公布。 公开号WO97 / 25082 日期:1997年8月14日由以下通式(1)表示的光学活性羟腈:其中R1和R2各自为氢原子或氨基保护基,并且与* 2位上的碳原子相关的构型 和* 3位如下:在*构型的* 2位的碳原子的情况下,* 3位的碳原子为S构型,在碳的情况下 在*构型的* 2位上的原子是3-构型的碳原子,可以通过使光学活性的氰醇中的一种结晶化,同时在存在的条件下处理氰醇非对映异构体的混合物 的胺和有机溶剂,以改变与2-位上的碳原子相关的构型,从而引起异构化。

    Etoposide phosphate and preparative intermediates
    5.
    发明授权
    Etoposide phosphate and preparative intermediates 失效
    依托泊甙磷酸盐和制备中间体

    公开(公告)号:US5606039A

    公开(公告)日:1997-02-25

    申请号:US410811

    申请日:1995-03-27

    IPC分类号: C07H17/04 C07H15/24

    CPC分类号: C07H17/04 Y02P20/55

    摘要: An etoposide phosphate represented by the formula (1): ##STR1## is prepared by blocking the hydroxyl groups of the saccharide moiety of etoposide with halogenoacetyl groups, thereafter phosphorylating the 4'-position, and removing the halogenoacetyl groups from the obtained phosphate in the presence of an amine.This process can give the objective etoposide phosphate in a higher yield than that of the prior art to enable the industrial mass-production thereof.

    摘要翻译: 由式(1)表示的依托泊苷磷酸酯:通过用卤代乙酰基封端依托泊苷的糖部分的羟基,然后磷酸化4'-位,并从得到的物质中除去卤代乙酰基来制备 磷酸盐在胺的存在下进行。 该方法可以使目标鬼臼乙叉甙磷酸盐以比现有技术更高的产率进行工业批量生产。