Title:
新規中間体を使用したボリコナゾールの製造方法
Document Type and Number:
Japanese Patent JP2013518876
Kind Code:
A
Abstract:
Provided is a process for preparing Voriconazole represented by Chemical Formula 1. More particularly, the process for preparing Voriconazole of Chemical Formula 1 includes: carrying out the Reformatsky-type coupling reaction between a ketone derivative of Chemical Formula 4 and a pyrimidine derivative of Chemical Formula 5 to obtain a compound of Chemical Formula 3; reacting the substituents halo and oxysulfonyl with a hydrogen donor to obtain racemic Voriconazole of Chemical Formula 2; and carrying out optical isolation of the racemic Voriconazole by adding an adequate optically active acid thereto to obtain Voriconazole having high optical purity with high cost-efficiency and high yield.
Inventors:
Kwon, Hyuk Chul
No man dong
Cha, Kyung Hee
No man dong
Cha, Kyung Hee
Application Number:
JP2012551915A
Publication Date:
May 23, 2013
Filing Date:
February 01, 2011
Export Citation:
Assignee:
Don Cook Pharmaceutical Company Limited
International Classes:
C07D403/10; A61K31/506; A61P31/10; C07B57/00; C07B61/00
Domestic Patent References:
| JPH04211078A | 1992-08-03 |
Foreign References:
| WO2009020323A2 | 2009-02-12 | |||
| WO2009024214A1 | 2009-02-26 | |||
| WO2009084029A2 | 2009-07-09 |
Attorney, Agent or Firm:
Kiyoji Kuzuwa