Sodium Chloride → HCID 66927248, compound

Participants

Reaction Steps

b-1.) To a suspension or solution of 2-(4-chlorophenyloxy)-4-chloro-5-trifluoromethylpyrimidine (e.g. 1.0 eq) and a suitable inorganic or organic auxiliary base, such as e.g. diisopropylethylamine, triethylamine or an alkali- or earth alkali-metal carbonate (e.g. sodium carbonate, e.g. 5 eq), in a suitable solvent, such as e.g. a solvent described herein as being suitable for nucleophilic aromatic substitution reactions (e.g. 1-methyl-2-pyrrolidinone [NMP]), an appropriate amine of formula V or a suitable salt thereof (e.g. 1.1 eq.) is added at low temperature, e.g. at 0° C. to 5° C. The reaction mixture is stirred under warming up to ambient temperature. The product can be isolated according to procedures familiar to the skilled person. An appropriate organic extractant, e.g. 2-methyl tetrahydrofurane, is added. After clearfiltration (if required), a 1 N sodium hydroxid solution and a saturated sodium chloride solution are added. The organic phase is separated and the solvent is evaporated under reduced pressure. The corresponding crude 2-(4-chlorophenyloxy)-4-amino-5-trifluoromethylpyrimidine derivative of formula IV is obtained as product which may contain NMP as residual solvent.

Provenance & Evidence