METHOD FOR PRODUCING FLUORINATED PROLINE DERIVATIVE
    2.
    发明公开
    METHOD FOR PRODUCING FLUORINATED PROLINE DERIVATIVE 审中-公开
    用于生产氟化脯氨酸衍生物

    公开(公告)号:EP1852419A4

    公开(公告)日:2009-03-04

    申请号:EP06712415

    申请日:2006-01-26

    IPC分类号: C07D207/16 C07D207/22

    CPC分类号: C07D207/16 C07D207/22

    摘要: Disclosed is a method for efficiently producing a high-purity fluorinated proline derivative with high yield. Specifically disclosed is a method for producing a compound represented by the general formula (2) below wherein a compound represented by the formula (1) below is reacted with a fluorination agent, and then chlorine, bromine, iodine, hypochlorous acid, hypochlorite, hypobromous acid, hypobromite or N-halogenosuccinimide is caused to act on the reaction product obtained by the preceding reaction and containing the compound represented by the general formula (2) below and a by-product for chemically changing the by-product. (1) (In the formula (1), R1 represents an unsubstituted or substituted alkyl group having 1-6 carbon atoms or the like; R2 represents an unsubstituted or substituted alkyl group having 1-6 carbon atoms or the like; and R3 represents a hydroxyl group or the like.) (2) (In the formula (2), R1 and R2 are as defined above.)

    OPTICALLY ACTIVE AZOLE DERIVATIVE AND PROCESS FOR PRODUCING THE SAME
    9.
    发明公开
    OPTICALLY ACTIVE AZOLE DERIVATIVE AND PROCESS FOR PRODUCING THE SAME 有权
    FOR光有源吡咯衍生物和方法及其

    公开(公告)号:EP1475370A4

    公开(公告)日:2005-07-13

    申请号:EP03706929

    申请日:2003-02-07

    摘要: A process for producing an optically active 2-phenyl-2,3-dihydroxypropylazole derivative which is a compound useful in the fields of medicines and agricultural chemicals and especially is an intermediate extremely important in the production of an antifungal agent of the optically active azole type; and novel intermediates obtained in the production process. An optically active α-hydroxycarboxylic acid derivative represented by the general formula (1) is reacted as a starting material with an azole acetic acid derivative (2) to produce an optically active novel azole alkyl ketone derivative (3). The derivative (3) is subjected to a highly diasteroselective alkylation reaction using a combination of a protective group with an organometallic reagent (4) to produce a novel, optically active azole methyl alcohol derivative (5). Furthermore, the protective group is selectively eliminated to produce an optically active 2-phenyl-2,3-dihydroxypropylazole derivative (6). general formula (1) neral formula (4) + + general formula (2) → general formula (3) → general formula (5) → general formula (6) Thus, a process for producing the optically active novel azole alkyl ketone derivative and the novel, optically active azole methyl alcohol derivative is provided. The optically active 2-phenyl-2,3-dihydroxypropylazole derivative can be stably produced at low cost through a small number of steps.