FIELD: pharmaceutical industry.
SUBSTANCE: present invention relates to a method for producing derivatives of 4-methoxypyrrol, which can be used to prevent or treat damage to the gastrointestinal tract due to ulcers of the gastrointestinal tract, gastritis, reflux esophagitis or Helicobacter pylori. The method includes the following stages: 1) the stage of obtaining a compound corresponding to chemical formula 4 given below by reacting a compound corresponding to chemical formula 2 given below with a compound corresponding to chemical formula 3 given below; 2) the stage of obtaining a compound corresponding to chemical formula 5 given below by reacting a compound corresponding to chemical formula 4 given below with sodium borohydride; 3) the stage of obtaining a compound corresponding to chemical formula 6 given below by reacting a compound corresponding to chemical formula 5 given below with an oxidizer; and 4) the reaction stage of a compound corresponding to chemical formula 6 given below with methylamine to obtain an intermediate, and converting the intermediate into a compound corresponding to chemical formula 1 given below by adding a reducing agent. In this case, the reaction temperature at stage 2 is from -15 to 80°C, oxidation at stage 3 is carried out in the presence of a mixture (diacetoxyiodo)benzene and (2,2,6,6-tetramethylpiperidine-1-yl)oxyl, and the reducing agent at stage 4 is sodium borohydride.
EFFECT: proposed method makes it possible, with the exclusion of hazardous and polluting reagents, to obtain target products with a high yield.
19 cl, 1 tbl, 3 ex
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Authors
Dates
2021-12-28—Published
2019-09-19—Filed