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    PROCESS FOR THE PREPARATION OF 1-(3,5-DICHLORO-4-FLUORO-PHENYL)-2,2,2-TRIFLUORO-ETHANONE
    1.
    发明申请
    PROCESS FOR THE PREPARATION OF 1-(3,5-DICHLORO-4-FLUORO-PHENYL)-2,2,2-TRIFLUORO-ETHANONE 有权

    公开(公告)号：US20170305828A1

    公开(公告)日：2017-10-26

    申请号：US15516087

    申请日：2015-10-08

    Applicant: SYNGENTA PARTICIPATIONS AG

    Inventor： Helmars SMITS

    IPC: C07C45/63 ,  C07C45/00 ,  C07C45/46 ,  C07C49/80

    CPC classification number: C07C45/63 ,  C07C45/004 ,  C07C45/46 ,  C07C49/80

    Abstract: The invention relates to a process for the preparation of a compound of formula I comprising a) reacting a compound of formula II in the presence of magnesium or an organometallic reagent of formula III R1M2X (III), wherein R1 is CI-C4alkyl; M2 is Li or Mg and X is halogen or absent; with a compound of formula IV CF3-C(O)-R2 (IV), wherein R2 is halogen, hydroxyl, CI-C4alkoxy, (di-CI-C4alkyl)amino, OC(O)CF3, phenoxy or OM1; wherein M1 is Lithium, Magnesium, Sodium or Potassium; to a compound of formula V, and b) reacting the compound of formula V with alkali metal fluoride in the presence of catalytic amounts of a phase transfer catalyst in the presence of a polar solvent to the compound of formula I.

    PROCESS FOR THE PREPARATION OF OPTICALLY ACTIVE ISOXAZOLINE COMPOUNDS
    2.
    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.

    PROCESS FOR THE PREPARATION OF SUBSTITUTED CYCLOSERINES
    7.
    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。

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