Process for the preparation of 5-(trifluoromethyl)-uracil, and the novel compounds 2,4-dichloro-5-trichloromethyl-pyrimidine and 2,4-difluoro-5-trifluoromethyl-pyrimidine

US5352787A · kind A · utility

Assignee

• BAYER HEALTHCARE LLC · DE

Inventors

• Peter Andres · Ginsheim-Gustavsburg, DE
• Albrecht Marhold · Leverkusen, DE

Key dates

• Filing date: Jul 2, 1993
• Grant date: Oct 4, 1994
• Expiry date: Jul 2, 2013

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D239/30
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

5-Trifluoromethyl-uracil is obtained by chlorinating thymine under mild conditions, further chlorinating the resulting 2,4-dichloro-5-methyl-pyrimidine under drastic conditions to give 2,4-dichloro-5-trichloromethylpyrimidine, reacting the latter with a fluorinating agent to give 2,4-fluorinated and/or -chlorinated 5- trifluoromethylpyrimidines and subjecting these to hydrolysis. The novel chemical compounds 2,4-dichloro- 5-trichloromethylpyrimidine and 2,4-difluoro-5-trifluoromethylpyrimidine are obtained in the course of this process.