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    AN IMPROVED PROCESS FOR THE PREPARATION OF ARMODAFINIL
    4.
    发明公开
    AN IMPROVED PROCESS FOR THE PREPARATION OF ARMODAFINIL 审中-公开
    改进制备方法阿莫达非尼的

    公开(公告)号：EP1954652A2

    公开(公告)日：2008-08-13

    申请号：EP07752169.8

    申请日：2007-03-01

    申请人： Teva Pharmaceutical Industries Ltd

    发明人： MOSHKOVITS-KAPTSAN, Rinat ,  BRAUDE, Viviana ,  CHEN, Kobi ,  ADLER, Miri

    IPC分类号： C07B57/00 ,  C07C315/06 ,  C07C317/44 ,  C07C319/24 ,  C07C321/20 ,  A61K31/192 ,  A61P25/00

    CPC分类号： C07C315/06 ,  C07B57/00 ,  C07B2200/07 ,  C07C319/24 ,  C07C317/44 ,  C07C321/20

    摘要： The invention encompasses processes for preparing intermediates, such as (R)-modafinic acid and its C1-2 alkyl ester, and the conversion of the intermediates into armodafinil. In particular, the invention concerns: (i) a process for the optical resolution of modafinic acid with (R)-α-naphthylethylamine and its conversion into armodafinil; (ii) (R)-modafinic acid containing less than 2% area by HPLC of (S)-modifinic acid; (iii) a process for the preparation of C1-2 alkyl ester of (R)-modafinic acid from (R)-modafinic acid by reaction with methanol or ethanol in the presence of at least one acidic reagent and its conversion into armodafinil; (iv) armodafinil with less than 0.5% area by HPLC of (S)-modafinil entantiomer, a pharmaceutical composition containing it and process for the preparation of this composition; (v) armodafinil with less than 0.1% area by HPLC of modafinic acid, a pharmaceutical composition containing it and process for the preparation of this composition; (vi) a process for the reduction of modafinic acid content in armodafjnil by contacting a solution with activated basic or neutral alumina; (vii) armodafinil with less than 0.2% area by HPLC of bis(diphenylmethyl) disulphide (R-MDF-DS), a pharmaceutical composition containing it and process for the preparation of this composition; (viii) a process for the preparation of R-MDF-DS from diphenylmethanethiol acetate; and (ix) a process for the reduction of R-MDF-DS content in armodafinil by suspending it in a C5-10 hydrocarbon.

    (E)-STYRYL SULFONE ANTICANCER AGENTS
    5.
    发明授权
    (E)-STYRYL SULFONE ANTICANCER AGENTS 有权
    （E） - 苯乙烯磺酸钠抗癌剂

    公开(公告)号：EP1173160B1

    公开(公告)日：2005-06-22

    申请号：EP00921553.4

    申请日：2000-03-31

    申请人： Temple University of the Commonwealth System of Higher Education

    发明人： REDDY, E., Premkumar ,  REDDY, M., V., Ramana

    IPC分类号： A61K31/10 ,  C07C317/10 ,  C07C321/20 ,  C07C317/44

    CPC分类号： C07C317/18 ,  C07C317/10 ,  C07C317/44

    摘要： (E)-styryl benzylsulfones of formula (I) are useful as anticancer agents wherein R1, R2, R3, and R4 are independently selected from the group consisting of hydrogen, fluoro, chloro, iodo, bromo, C1-C6 alkyl, C1-C4 alkoxy, nitro, cyano and trifluoromethyl, with the proviso that (a) R1, R2, and R3 not all hydrogen when R4 is 2-chloro or 4-chloro; (b) when R1 and R3 are hydrogen and R2 is 4-bromo or 4-chloro, then R4 may not be 4-chloro, 4-fluoro or 4-bromo; (c) when R1 and R3 are hydrogen and R2 is 4-fluoro, then R4 may not be 4-fluoro or 4-bromo; (d) when R1 is hydrogen, and R4 is 2-fluoro, the R2 and R3 may not be 4-fluoro; and (e) when R1 is hydrogen and R3 is 4-hydrogen, 4-chloro, 4-bromo, 4-methyl or 4-methoxy, and R4 is 2-hydrogen, 2-chloro, or 2-fluoro; then R2 may not be 4-hydrogen, 4-chloro, 4-fluoro, or 4-bromo.

    摘要翻译： （E） - 苯乙烯基苄基砜可用作抗癌剂，其中R 1，R 2，R 3和R 4独立地选自氢，氟，氯，碘，溴，C 1 -C 6烷基，C 1 -C 6烷基， C4烷氧基，硝基，氰基和三氟甲基，条件是（a）当R4是2-氯或4-氯时，R1，R2和R3不全是氢; （b）当R 1和R 3是氢并且R 2是4-溴或4-氯时，则R 4可以不是4-氯，4-氟或4-溴; （c）当R 1和R 3是氢并且R 2是4-氟时，则R 4可以不是4-氟或4-溴; （d）当R 1为氢且R 4为2-氟时，R 2和R 3可以不是4-氟; 和（e）当R 1为氢且R 3为4-氢，4-氯，4-溴，4-甲基或4-甲氧基，且R 4为2-氢，2-氯或2-氟时; 那么R2可能不是4-氢，4-氯，4-氟或4-溴。