FIELD: medicine; pharmaceutics; chemistry.
SUBSTANCE: invention relates to pharmaceutical and organic chemistry, specifically to synthesis of selexipag, which has found application for treating pulmonary arterial hypertension. Method of production is characterized by that synthesis is carried out in two steps, where at the first step, when reacting 5-chloro-2,3-diphenylpyrazine with 4-isopropylamino-1-butanol in the presence of an alkali metal iodide, 4-[N-(5,6-diphenylpyrazin-2-yl)-N-isopropylamino]-1-butanol. First step is carried out without using catalysts and solvents, as well as without isolating intermediate 6-iodo-2,3-diphenylpyrazine. Second step is carried out by reacting 4-[N-(5,6-diphenylpyrazin-2-yl)-N-isopropylamino]-1-butanol with 2-chloro-N-(methylsulphonyl)acetamide.
EFFECT: reduction of process steps, performance of a key step in the absence of solvents and increased output and purity of the end product.
6 cl, 6 ex
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Authors
Dates
2025-04-22—Published
2023-08-04—Filed