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    PROCESS FOR THE PREPARATION OF BIMATOPROST
    6.
    发明申请
    PROCESS FOR THE PREPARATION OF BIMATOPROST 审中-公开

    公开(公告)号：US20200010406A1

    公开(公告)日：2020-01-09

    申请号：US16090572

    申请日：2017-04-18

    Applicant: GENTEC, S.A.

    Inventor： Luis Octavio SILVA GUISASOLA ,  Joaquín NEBOT TROYANO ,  Jordi RIPOLL ALTADILL

    IPC: C07C231/14 ,  C07C67/04 ,  C07C69/608 ,  C07C233/10

    Abstract: It is provided a process for the preparation of bimatoprost, which comprises: a) reacting a compound of formula (III) with ethylamine in the presence of a suitable solvent; and b) deprotecting compound obtained in step a) to obtain bimatoprost, wherein R1 is selected from (C1-C16)alkyl, (C1C16)haloalkyl, (C2-C16)alkenyl, (C2-C16)haloalkenyl, (C1-C16)alkoxy(C1-C16)alkyl, aryl, (C1-C16)alkylaryl, allyl, —(CH2—CH2—O)n—CH3 wherein n=1, 2, 3 or 4, and —CH(O—CH2—CH2)2; R2 is selected from H, (C1-C16)alkyl, (C1-C16)haloalkyl, (C2-C16)alkenyl, (C2-C16)haloalkenyl, (C1-C16)alkoxy(CrC16)alkyl, aryl, (C1-C16)alkylaryl, allyl; or, alternatively, R1 and R2 taken together are selected from —CH2—CH2—CH2—, —CH2—CH2—, —O—CH2—CH2—, and —O—CH═CH—. There are also provided intermediates useful in such preparation process.

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