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Title:
PROCESS FOR PREPARATION OF TOLTERODINE AND ITS L-TARTRATE
Document Type and Number:
WIPO Patent Application WO/2010/078703
Kind Code:
A1
Abstract:
The invention provides a process for the preparation of Tolterodine and its L-tartrate.  The preparation is as follows, A) after diisopropyl amine is activated by activator, it is reacted with 3,4-dihydro-6-methyl-4-phenylchroman-2-one to obtain N,N-diisopropyl-3-phenyl-3-(2-hydroxy-5-methylphenyl)-propionamide; or after diisopropyl amine and 3,4-dihydro-6-methyl-4-phenyl-chroman-2-one are actived by Lewis acid, they take aminolysis to obtain N,N-diisopropyl-3-phenyl-(2-hydroxy-5-methylphenyl)-propionamide; B) N,N-diisopropyl-3-phenyl-(2-hydroxy-5-methylphenyl)-propionamide is reduced by reductant to obtain the free base of (±)-Tolterodine; C) the free base of (±)-Tolterodine was resolved by L-(+)-tartaric acid to give L-(+)-Tolterodine tartrate. The process has the advantages of simple procedure, low cost, high yield, easy to operate, simple post-treatment, steady quality of the product, and suitable for industrial production.

Inventors:
WANG GANG (CN)
ZHANG JINGZHONG (CN)
HE XUNGUI (CN)
WANG YUAN (CN)
Application Number:
PCT/CN2009/000950
Publication Date:
July 15, 2010
Filing Date:
August 18, 2009
Export Citation:
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Assignee:
2Y CHEM LTD (CN)
WANG GANG (CN)
ZHANG JINGZHONG (CN)
HE XUNGUI (CN)
WANG YUAN (CN)
International Classes:
C07C215/54; A61P13/00; A61P13/06; C07C213/00; C07C213/10
Domestic Patent References:
WO2008020332A22008-02-21
Foreign References:
CN101445462A2009-06-03
CN1903833A2007-01-31
Other References:
CHEN, GANG ET AL.: "Rhodium-Catalyzed Asymmetric 1,4-Addition of Arylboronic Acids to Coumarins: Asymmetric Synthesis of (R)-Tolterodine", ORGANIC LETTERS, vol. 7, no. 11, 2005, pages 2285 - 2288
Attorney, Agent or Firm:
KINGSOUND & PARTNERS (Block BKingSound International Center,116 Zizhuyuan Road,Haidian District, Beijing 7, CN)
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