Title:
Ｒ（＋）α−リポ酸の合成
Document Type and Number:
Japanese Patent JP4257574
Kind Code:
B2
Abstract:
Process for the synthesis of R(+)alpha-lipoic acid comprising the following stages: a) Salifying of racemic 6,8-halo-octanoic acid with S(-)alpha-methylbenzylamine; b) separation by filtration of the crystallized diastereoisomeric salt of R(+)6,8-di-halo-octanoic acid-S(-)alpha-methylbenzylamine; c) purification by re-crystallization of the diastereoisomeric salt of R(+)6,8-di-halo-octanoic acid-S(-)alpha-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(+)alpha-lipoic acid.
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Inventors:
ヴィルラニ・フラヴィオ
サルヴィ・アンニバーレ
ナルディ・アントニオ
ファラベッラ・ジオヴァンナ
サルヴィ・アンニバーレ
ナルディ・アントニオ
ファラベッラ・ジオヴァンナ
Application Number:
JP2002534305A
Publication Date:
April 22, 2009
Filing Date:
October 08, 2001
Export Citation:
Assignee:
ラボラトリオ チミコ インターナジオナーレ ソシエタ ペル アチオニ
International Classes:
C07D339/04; C07B53/00; C07B57/00; C07B61/00; C07C51/41; C07C51/487; C07C53/19; C07C67/08; C07C69/63
Attorney, Agent or Firm:
山下 穣平