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    PROCESS FOR THE PREPARATION OF SUBSTITUTED CYCLOSERINES
    1.
    发明申请
    PROCESS FOR THE PREPARATION OF SUBSTITUTED CYCLOSERINES 有权
    制备取代环孢霉素的方法

    公开(公告)号：US20170044116A1

    公开(公告)日：2017-02-16

    申请号：US15307386

    申请日：2015-04-30

    Applicant: Syngenta Participations AG

    Inventor： Tomas SMEJKAL ,  Helmars SMITS ,  Christian LOTHSCHUETZ ,  Miroslav TERINEK

    IPC: C07D261/04

    CPC classification number: C07D261/04 ,  C07C259/06 ,  C07D261/12

    Abstract: The present invention relates to processes for the preparation of substituted cycloserine compounds of formula (I) wherein R1 is C1-C8alkyl, C1-C8haloalkyl, C3-C6cycloalkyl, aryl or aryl substituted by one to five R11, or aryl-C1-C4alkylene or aryl-C1-C4alkylene substituted by one to five R11; and each R11 is independently C1-C4alkyl, C1-C4haloalkyl, C1-C4alkoxy, C1-C4haloalkoxy, cyano or halogen; The invention also relates to intermediates produced by the processes. Compounds of formula (I) are useful intermediates for the production of compounds in the agricultural and pharmaceutical fields.

    Abstract translation: 本发明涉及制备式（I）的取代环丝氨酸化合物的方法，其中R 1是C 1 -C 8烷基，C 1 -C 8卤代烷基，C 3 -C 6环烷基，被1至5个R 11取代的芳基或芳基或芳基-C 1 -C 4亚烷基或 被一至五个R 11取代的芳基-C 1 -C 4亚烷基; 每个R 11独立地为C 1 -C 4烷基，C 1 -C 4卤代烷基，C 1 -C 4烷氧基，C 1 -C 4卤代烷氧基，氰基或卤素; 本发明还涉及通过该方法制备的中间体。 式（I）化合物是农业和制药领域中化合物生产的有用中间体。

    PROCESS FOR THE PREPARATION OF OPTICALLY ACTIVE ISOXAZOLINE COMPOUNDS
    6.
    发明申请
    PROCESS FOR THE PREPARATION OF OPTICALLY ACTIVE ISOXAZOLINE COMPOUNDS 有权

    公开(公告)号：US20170217953A1

    公开(公告)日：2017-08-03

    申请号：US15501008

    申请日：2015-08-04

    Applicant: SYNGENTA PARTICIPATIONS AG

    Inventor： Tomas SMEJKAL ,  Helmars SMITS

    IPC: C07D453/04 ,  B01J31/02 ,  C07D261/14

    CPC classification number: C07D453/04 ,  B01J31/02 ,  B01J31/0244 ,  C07B53/00 ,  C07D261/08 ,  C07D261/14

    Abstract: The present invention relates to a process for the preparation of a compound of formula (I) wherein A1 and A2 are C—H, or one of A1 and A2 is C—H and the other is N; R1 is C1-C4alkyl, C1-C4haloalkyl or C3-C6cycloalkyl; each R2 is independently bromo, chloro, fluoro or trifluoromethyl; R3 is hydrogen; R4 is hydrogen, halogen, methyl, halomethyl or cyano; or R3 and R4 together form a bridging 1,3-butadiene group; R5 is chlorodifluoro-methyl or trifluoromethyl; n is 2 or 3; by reacting a compound of formula (II) wherein A1, A2, R1, R2, R3, R4, R5 and n is as defined under formula (I) above, with hydroxylamine, a base and a chiral catalyst, characterized in that the chiral catalyst is a dimeric chiral catalyst of formula (III) wherein R6, R7, R8, R9, R10 and X are as defmed in claim 1.

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