发明名称 |
AN IMPROVED PROCESS FOR THE PREPARATION OF ARMODAFINIL |
摘要 |
The invention encompasses processes for preparing intermediates, such as (R)-modafinic acid and its C<SUB>1-2</SUB> 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)-a-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 C<SUB>1-2</SUB> 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 C<SUB>5-10</SUB> hydrocarbon. |
申请公布号 |
WO2007103221(A3) |
申请公布日期 |
2008.06.26 |
申请号 |
WO2007US05451 |
申请日期 |
2007.03.01 |
申请人 |
TEVA PHARMACEUTICAL INDUSTRIES LTD.;TEVA PHARMACEUTICALS USA, INC.;MOSHKOVITS-KAPTSAN, RINAT;BRAUDE, VIVIANA;CHEN, KOBI;ADLER, MIRI |
发明人 |
MOSHKOVITS-KAPTSAN, RINAT;BRAUDE, VIVIANA;CHEN, KOBI;ADLER, MIRI |
分类号 |
C07B57/00;A61K31/192;A61P25/00;C07C315/06;C07C317/44;C07C319/24;C07C321/20 |
主分类号 |
C07B57/00 |
代理机构 |
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代理人 |
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主权项 |
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地址 |
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