发明授权
- 专利标题: SYNTHESIS OF R(+)ALPHA-LIPOIC ACID
- 专利标题(中): 的R的合成 - (+) - α-硫辛酸
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申请号: EP01986686.2申请日: 2001-10-08
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公开(公告)号: EP1335911B1公开(公告)日: 2004-05-06
- 发明人: VILLANI, Flavio, Lab. Chimico InternationalS.p.A. , NARDI, Antonio, Lab. Chimico Internazional S.p.A. , SALVI, Annibale, Lab. Chimico Internazional S.p.A. , FALABELLA, G., Lab. Chimico Internazional S.p.A.
- 申请人: LABORATORIO CHIMICO INTERNAZIONALE S.p.A.
- 申请人地址: Via Salvini, 10 20122 Milano IT
- 专利权人: LABORATORIO CHIMICO INTERNAZIONALE S.p.A.
- 当前专利权人: LABORATORIO CHIMICO INTERNAZIONALE S.p.A.
- 当前专利权人地址: Via Salvini, 10 20122 Milano IT
- 代理机构: Gervasi, Gemma, Dr.
- 优先权: ITMI20002188 20001010
- 国际公布: WO2002030919 20020418
- 主分类号: C07D339/04
- IPC分类号: C07D339/04
摘要:
Process for the synthesis of R(+)α-lipoic acid comprising the following stages: a) Salifying of racemic 6,8-halo-octanoic acid with S(-)α-methylbenzylamine; b) separation by filtration of the crystallized diastereoisomeric salt of R(+)6,8-di-halo-octanoic acid-S(-)α-methylbenzylamine; c) purification by re-crystallization of the diastereoisomeric salt of R(+)6,8-di-halo-octanoic acid-S(-)α-methylbenzylamine; d) separation of the diastereoisomeric salt to obtain R(+)6,8-di-halo-octanoic acid by reation of said salt with strong mineral acids in an aqueous solution with a dilution between 2 and 10% by weight; e) esterification of R(+)6,8-di-halo-octanoic acid to obtain the corresponding alkyl ester; f) reaction of the alkyl ester of R(+)6,8-di-halo-octanoic acid in an organic solvent with an aqueous solution of alkali disulfide in presence of a compound for phase transfer catalysis; g) hydolysis of the ester of R(+)α-lipoic acid.
公开/授权文献
- EP1335911A1 SYNTHESIS OF R(+)ALPHA-LIPOIC ACID 公开/授权日:2003-08-20
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