15-09-2022 дата публикации
Номер: US20220289684A1
Принадлежит:
The present disclosure relates to a benzimidazole-substituted phenyl-n-butyramide-based compound and the preparation method thereof. The method of the present disclosure avoids nitration reaction and polyphosphoric acid cyclization reaction, and avoids the generation of a large amount of waste acid reaction solution from the source. The synthesis method embodied in the invention has the advantages of simplicity and high efficiency, mild conditions and few pollutants, etc., and is suitable to be developed as a green and sustainable production process. 4. The method according to claim 2 , wherein the method Five is conducted according to one of the following three methods:{'sub': '3', 'Method (a), when Ris chlorine, or bromine, or n-butyryloxy, reacting the compound of formula VI with n-butyryl chloride, or n-butyryl bromide, or n-butyric anhydride to prepare the compound of formula III,'}In particular, method (a) is conducted in presence of a basic reagent, the basic reagent is one selected from the group consisting of lithium carbonate, sodium carbonate, potassium carbonate, cesium carbonate, sodium bicarbonate, potassium bicarbonate, sodium phosphate, potassium phosphate, sodium monohydrogen phosphate, potassium monohydrogen phosphate, lithium hydroxide, sodium hydroxide, potassium hydroxide, magnesium carbonate, magnesium hydroxide, calcium carbonate, calcium hydroxide, calcium oxide, magnesium oxide, lithium methoxide, sodium methoxide, potassium methoxide, sodium ethoxide, potassium ethoxide, lithium isopropoxide, sodium isopropoxide, potassium isopropoxide, lithium tert-butoxide, sodium tert-butoxide, potassium tert-butoxide, magnesium methoxide, magnesium ethoxide, magnesium tert-butoxide, ammonia water, triethylamine, diisopropylamine, diisopropyl ethyl amine, tri-n-butyl amine, pyridine, 2-methylpyridine, 2,6-dimethylpyridine, 4-dimethylaminopyridine, tetrahydropyrrole, morpholine, piperidine and 2,2,6,6-tetramethylpiperidine; or a mixture thereof;In ...
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