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Title:
S-インドリン-2-カルボン酸を合成する新規な方法、およびペリンドプリルの合成におけるその適用
Document Type and Number:
Japanese Patent JP5111849
Kind Code:
B2
Abstract:
Process for industrial synthesis of (2S) indoline-2-carboxylic acid (I) by reacting racemic acid (III) with chiral amine to form salts (IV), separating crystals of (2S) salt from (2R) salt and then: (1) acidifying (2S) salt of (IV) to give (I); and (2) acidifying (2R) salt of (IV) to form a mixture having a majority of the (2R) acid, racemizing this to form (III) and repeating the process. Process for the industrial synthesis of (2S) indoline-2-carboxylic acid of formula (I) comprises: (1) reacting the racemic acid of formula (III) with a chiral amine to form the salts of formulae (IVa) and (IVb); (2) separating crystals of the (2S) salt (IVa) from the (2R) salt (IVb); (3) acidifying (IVa) with hydrochloric acid (HCl) to form (I); and (4) acidifying the residue containing the (2R) salt (IVb) with HCl to form a mixture having a majority of the (2R) acid; (5) racemizing this with the sodium hydroxide to form the racemic acid (III); and (6) repeating the process. An Independent claim is also included for preparation of perindopril using (I) prepared by the described process.

Inventors:
Svi, Jean-Claude
Lukve, Jean-Pierre
Application Number:
JP2006500165A
Publication Date:
January 09, 2013
Filing Date:
April 07, 2004
Export Citation:
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Assignee:
Réra Bora Toir Servier
International Classes:
C07D209/42; C07B55/00; C07B57/00
Domestic Patent References:
JP1110696A
JP6142A
JP6354346A
JP2124881A
JP469356A
JP5549059B2
JP58216147A
JP1511742A
Attorney, Agent or Firm:
Hajime Tsukuni
Fusayuki Saito
Yoko Tanaka



 
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