Title:
4,6-ジクロロ-5-フルオロピリミジンを製造する方法
Document Type and Number:
Japanese Patent JP5279156
Kind Code:
B2
Abstract:
Preparation of 4,6-dichloro-5-fluoro-pyrimidine (I) involves: (a) reacting a fluoromalonic acid diester (II) with formamide in presence of an alkali metal alkoxide and optionally acidifying; and (b) reacting the obtained 4,6-dihydroxy-5-fluoropyrimidine (III) or its alkali metal salt with phosphorus oxychloride, reacting with chlorine in presence of phosphorus trichloride and working up by distillation, such that (I) is separated and phosphorus oxychloride is recycled. Preparation of 4,6-dichloro-5-fluoro-pyrimidine of formula (I) involves: (a) reacting a fluoromalonic acid diester of formula (II) with formamide, in presence of an alkali metal alkoxide and optionally a diluent, at elevated temperature and optionally elevated pressure, and optionally acidifying the reaction mixture; and (b) reacting the obtained 4,6-dihydroxy-5-fluoropyrimidine of formula (III) or its alkali metal salt (optionally without isolation) with phosphorus oxychloride, reacting the obtained reaction mixture with chlorine in presence of phosphorus trichloride such that at most 99.9 wt. % of the chlorophosphonic acid present in the reaction mixture is converted and working up the obtained reaction mixture by distillation, such that the obtained (I) is separated and phosphorus oxychloride is recycled. R = Me or Et.
Inventors:
Holger Bainlitt
Reinhard Ranchille
Reinhard Ranchille
Application Number:
JP2000241073A
Publication Date:
September 04, 2013
Filing Date:
August 09, 2000
Export Citation:
Assignee:
Bayer Aktiengesellschaft
International Classes:
C07D239/30; A01N43/54; C07D239/54
Domestic Patent References:
| JP61205262A | ||||
| JP967351A | ||||
| JP1067755A |
Foreign References:
| WO1998041513A2 |
Attorney, Agent or Firm:
Patent business corporation Odashima patent office