FIELD: chemistry.
SUBSTANCE: invention relates to a novel process for the preparation of 2-trifluoromethylisonicic acid and its ethers of the formula I
,
where R1 is hydrogen or C1-6-alkyl, according to which the conversion of a 2-trifluoromethylpyridine derivative of the formula II is performed
,
where X is halogen or -OSO2CY3, where Y is halogen, with carbon monoxide (CO) in the presence of the reagent R1OH, in the presence of a palladium complex catalyst selected from palladium (II) chloride with ligand 1.1'-bis(diphenylphosphino)ferrocene (DPPF).
.
EFFECT: trifluoromethylisonicicinic acid and its esters of the formula I are variable intermediates for the preparation of active pharmaceutical agents and agrochemicals such as, for example, TAAR1 agonists of the formula III.
12 cl, 12 ex
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Authors
Dates
2018-05-21—Published
2013-11-13—Filed