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    AN IMPROVED PROCESS FOR THE PREPARATION OF CLARITHROMYCIN
    2.
    发明申请
    AN IMPROVED PROCESS FOR THE PREPARATION OF CLARITHROMYCIN 审中-公开
    改进氯雷他定的制备方法

    公开(公告)号：WO2009023191A2

    公开(公告)日：2009-02-19

    申请号：PCT/US2008/009633

    申请日：2008-08-11

    Applicant: TEVA PHARMACEUTICAL INDUSTRIES LTD. ,  TEVA PHARMACEUTICALS USA, INC. ,  KANSAL, Vinod, Kumar ,  MISTRY, Dhirenkumar, N. ,  GANDHI, Mitesh ,  PATEL, Rakesh

    Inventor： KANSAL, Vinod, Kumar ,  MISTRY, Dhirenkumar, N. ,  GANDHI, Mitesh ,  PATEL, Rakesh

    CPC classification number: C07H17/08 ,  C07H1/00

    Abstract: The present invention includes a process involving a one-pot reaction for preparing erythromycin 9-oxime salt comprising: (a) reacting erythromycin thiocyanate with an ammonium source to obtain erythromycin free base; (b) oximating the C-9 carbonyl of the erythromycin free base by reacting the erythromycin free base with triethylamine and hydroxyl amine hydrochloride to form erythromycin oxime; and (c) reacting the erythromycin oxime obtained in step (b) with an ammonium source to obtain the erythromycin 9-oxime salt. The present invention is also drawn to a one-pot reaction for preparing clarithromycin starting with the one-pot reaction for preparing erythromycin 9-oxime salt, further comprising after step (c): (d) silylating the hydroxy groups at the oxime group, and the 2" and 4> λ positions of the erythromycin 9-oxime salt to obtain a silylated derivative; (e) methylating the hydroxy group at the 6 position of the silylated derivative using at least one methylating agent in the presence of at least one inorganic base to obtain SMOP, wherein SMOP is 6-O-methyl-2', 4"-bis(trimethylsilyl)- erythromycin A 9-O-(2-methoxyprop-2-yl)oxime; and (f) converting the SMOP into clarithromycin using at least one deoximating agent in the presence of aqueous ethanol.

    Abstract translation: 本发明包括一种用于制备红霉素9-肟盐的一锅反应的方法，包括：（a）将红霉素硫氰酸盐与铵源反应以获得游离红霉素的碱; （b）通过使红霉素游离碱与三乙胺和羟胺盐酸盐反应，使红霉素游离碱的C-9羰基肟化，形成红霉素肟; 和（c）使步骤（b）中获得的红霉素肟与铵源反应，得到红霉素9-肟盐。 本发明还涉及从用于制备红霉素9-肟盐的一锅反应开始制备克拉霉素的一锅反应，还包括在步骤（c）之后：（d）使肟基上的羟基甲硅烷基化， 和红霉素9-肟盐的2“和4”→位置，以获得甲硅烷基化衍生物;（e）使用至少一种甲基化试剂在甲硅烷基化衍生物的6位甲基化存在下， 无机碱以获得SMOP，其中SMOP为6-O-甲基-2'，4“ - 双（三甲基甲硅烷基） - 红霉素A 9-O-（2-甲氧基丙-2-基）肟; 和（f）在含水乙醇的存在下使用至少一种去肟剂将SMOP转化成克拉霉素。

    AN IMPROVED PROCESS FOR THE PREPARATION OF CLARITHROMYCIN
    4.
    发明申请
    AN IMPROVED PROCESS FOR THE PREPARATION OF CLARITHROMYCIN 审中-公开
    一种改进的克拉霉素制备方法

    公开(公告)号：WO2009023191A3

    公开(公告)日：2009-04-23

    申请号：PCT/US2008009633

    申请日：2008-08-11

    Applicant: TEVA PHARMA ,  TEVA PHARMA ,  KANSAL VINOD KUMAR ,  MISTRY DHIRENKUMAR N ,  GANDHI MITESH ,  PATEL RAKESH

    Inventor： KANSAL VINOD KUMAR ,  MISTRY DHIRENKUMAR N ,  GANDHI MITESH ,  PATEL RAKESH

    IPC: C07H1/00 ,  A61K31/7048 ,  A61P31/04 ,  C07H17/08

    CPC classification number: C07H17/08 ,  C07H1/00

    Abstract: The present invention includes a process involving a one-pot reaction for preparing erythromycin 9-oxime salt comprising: (a) reacting erythromycin thiocyanate with an ammonium source to obtain erythromycin free base; (b) oximating the C-9 carbonyl of the erythromycin free base by reacting the erythromycin free base with triethylamine and hydroxyl amine hydrochloride to form erythromycin oxime; and (c) reacting the erythromycin oxime obtained in step (b) with an ammonium source to obtain the erythromycin 9-oxime salt. The present invention is also drawn to a one-pot reaction for preparing clarithromycin starting with the one-pot reaction for preparing erythromycin 9-oxime salt, further comprising after step (c): (d) silylating the hydroxy groups at the oxime group, and the 2" and 4> ? positions of the erythromycin 9-oxime salt to obtain a silylated derivative; (e) methylating the hydroxy group at the 6 position of the silylated derivative using at least one methylating agent in the presence of at least one inorganic base to obtain SMOP, wherein SMOP is 6-O-methyl-2', 4"-bis(trimethylsilyl)- erythromycin A 9-O-(2-methoxyprop-2-yl)oxime; and (f) converting the SMOP into clarithromycin using at least one deoximating agent in the presence of aqueous ethanol.

    Abstract translation: 本发明包括涉及制备红霉素9-肟盐的一锅法反应的方法，其包括：（a）使硫氰酸红霉素与铵源反应以获得红霉素游离碱; （b）通过使红霉素游离碱与三乙胺和羟胺盐酸盐反应形成红霉素肟来肟化红霉素游离碱的C-9羰基; 和（c）使步骤（b）中得到的红霉素肟与铵源反应得到红霉素9-肟盐。 本发明还涉及用制备红霉素9-肟盐的一锅法反应制备克拉霉素的一锅法反应，在步骤（c）之后进一步包括：（d）将肟基上的羟基甲硅烷基化， 和红霉素9-肟盐的2'和4''位以获得甲硅烷基化衍生物;（e）使用至少一种甲基化试剂，在至少一种存在下甲基化甲硅烷基化衍生物的6位上的羟基 SMOP是6-O-甲基-2'，4“ - 双（三甲基甲硅烷基） - 红霉素A 9-O-（2-甲氧基丙-2-基）肟; 和（f）使用至少一种脱氧剂在含水乙醇存在下将SMOP转化为克拉霉素。

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