- Preparation method of 3-alkyl-5-trifluoromethylaniline
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The invention discloses an effective synthesis method of 3-alkyl -5-trifluoromethylaniline. The method comprises an alkylation reaction and a reduction reaction. According to the alkylation reaction,a compound II 3-bromine -5-nitro benzotrifluoride and alkyl boric acid are used as substrates and react in dioxane at 100 DEG C in a nitrogen environment under the conditions of a palladium catalyst and a potassium carbonate aqueous solution to obtain an alkylation product as shown in a structural general formula III. And reduction reaction is carried out, namely dissolving the compound III serving as a substrate in ethanol at 80 DEG C under the condition of zinc and concentrated hydrochloric acid, and reacting to obtain the 3-alkyl- 5-trifluoromethylaniline shown in the structural general formula I. The method is economical, and the substrates 3-bromine -5-nitro benzotrifluoride and alkyl boric acid reagents are very cheap; acid is not needed in the alkylation step, and environmental friendliness is achieved; the alkylation reaction yield is high, and the product I can be subjected to gram-grade preparation.
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Paragraph 0034-0035
(2020/12/30)
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