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    A PROCESS FOR DIMETHYLATION OF ACTIVE METHYLENE GROUPS
    3.
    发明公开
    A PROCESS FOR DIMETHYLATION OF ACTIVE METHYLENE GROUPS 审中-公开
    方法二甲基化活性甲基基团

    公开(公告)号：EP2414320A1

    公开(公告)日：2012-02-08

    申请号：EP10711884.6

    申请日：2010-03-30

    Applicant: LEK Pharmaceuticals d.d.

    Inventor： JENKO, Branko ,  COPAR, Anton

    IPC: C07C231/12 ,  C07C253/30 ,  C07C255/19 ,  C07C237/06 ,  A61K31/275 ,  A61K31/16

    CPC classification number: C07C253/30 ,  C07C231/12 ,  C07C237/06 ,  C07C255/19

    Abstract: The present invention discloses a process for dimethylation of active methylene groups. Specifically, the invention discloses aprocess for preparing3-amino-2,2- dimethylpropanamide. Compounds produced by the present dimethylation process such as 3-amino-2,2-dimethylpropanamide can be used as intermediates in the route of synthesis of therapeutic, prophylactic or diagnostic agent, for example aliskiren or cryptophycin. Particularly, the invention relates to embodiments further extending to processesfor preparing pharmaceutical dosage form comprising said therapeutic, prophylactic or diagnostic agents. More specifically, the invention relates to the use of compounds produced by the present dimethylation process for the manufacture of therapeutic, prophylactic or diagnostic agents or for the manufacture of pharmaceutical dosage forms comprising said therapeutic, prophylactic or diagnostic agents. The processes according to the present invention can be beneficially applied for the synthesis of various active pharmaceutical ingredients, such as aliskiren or crypthophycin.

    2'-HALOBIPHENYL-4-YL INTERMEDIATES IN THE SYNTHESIS OF ANGIOTENSIN II ANTAGONISTS
    4.
    发明公开
    2'-HALOBIPHENYL-4-YL INTERMEDIATES IN THE SYNTHESIS OF ANGIOTENSIN II ANTAGONISTS 有权
    2'-卤代联-4-基 - 中间体在血管紧张素II拮抗剂的合成

    公开(公告)号：EP2279159A2

    公开(公告)日：2011-02-02

    申请号：EP09723165.8

    申请日：2009-03-19

    Applicant: LEK Pharmaceuticals d.d.

    Inventor： COPAR, Anton ,  CASAR, Zdenko ,  PREMRL, Andrej

    IPC: C07C17/26 ,  C07C25/18 ,  C07D235/18

    CPC classification number: C07C17/263 ,  C07C17/14 ,  C07C17/2632 ,  C07D235/20 ,  Y10T436/147777 ,  C07C25/18

    Abstract: A process for obtaining 2'-halo-4-methylbiphenyls is described, which comprises reacting 4 halotoluene with a 1,2-dihalobenzene in the presence of elemental metal such as magnesium, lithium or zinc, wherein 0 to 0.9 molar, particularly 0 to 0.2 molar excess of 4-halotoluene in regard to 1,2-dihalobenzene is used, and arised organometal intermediates are quenched by elemental halogen. In addition, the coupling of arised 2'-halo-4-methylbiphenyls with 2-(1-propyl)-4-methyl-6-(1'-methylbenzimidazole-2-il)benzimidazole to afford 3'-(2'-halo-biphenyl-4-ylmethyl)-1,7'-dimethyl-2'-propyl-1H,3'H-[2,5']bibenzoimidazolyl, which can be further converted to organometallic compound and said organometallic compound is further reacted with formic acid derivative, such as N,N-dimethylformamide, alkylformiate or carbon dioxide to obtain telmisartan, is also described. Further described is use of in line analytics for monitoring the aforementioned reactions, process for preparing a pharmaceutical composition and/or dosage for, or use in preparing a medicament.

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