3932-97-6Relevant articles and documents
Method for preparing 5-trifluoromethyl uracil
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Paragraph 0036-0037, (2019/06/05)
The invention belongs to the field of organic synthesis, and specifically relates to a method for preparing 5-trifluoromethyl uracil. The method comprises the following steps: firstly, carrying out chlorination reaction on 5-iodouracil and phosphorus oxychloride, thus obtaining 2,4-dichloro-5-iodopyrimidine; secondly, carrying out trifluoromethylation reaction on the 2,4-dichloro-5-iodopyrimidineand a trifluoromethylating reagent, thus obtaining 2,4-dichloro-5-trifluoromethylpyrimidine; finally, enabling the 2,4-dichloro-5-trifluoromethylpyrimidine to react with acetic acid, thus obtaining aproduct. According to the method disclosed by the invention, since chlorination reaction, trifluoromethylation reaction and hydrolysis reaction are adopted, a key intermediate-trifluoromethyl uracil of trifluorothymidine is synthesized in high yield, low cost and low pollution.
Trifluoroethoxy group as a leaving group for regioselective sequential substitution reactions of 5-trifluoromethylpyrimidine derivative with heteroatom nucleophiles
Kagawa, Takumi,Shigehiro, Daiki,Kawada, Kosuke
, p. 150 - 158 (2015/11/10)
Highly regioselective substitution reaction of 2,4-bis(2,2,2-trifluoroethoxy)-5-(trifluoromethyl)pyrimidine (TFEFP) with aniline derivatives smoothly proceeded firstly at the 2-postion. For the subsequent nucleophilic substitution at the 4-position with alkoxides, trifluoroethoxy group at the 4-position serves as a practically efficient leaving group.
SYNTHESIS OF 2,4-DICHLORO-5-TRIFLUOROMETHYL-PYRIMIDINE
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Paragraph 0060; 0061; 0062; 0063; 0064, (2014/05/20)
This invention relates to a novel method for the synthesis of 2,4-dichloro-5-trifluoromethyl-pyrimidine useful as intermediate in the manufacture of pharmaceutically active ingredients.