4-Hydroxy-1-methyl-7-phenoxy-3-isoquinolinecarboxylic acid methyl ester

Uses

4-Hydroxy-1-methyl-7-phenoxy-methyl ester-3-isoquinolinecarboxylic Acid is used as a reagent in the preparation of Roxadustat (H948180), which is a drug used to treat anemia and chronic renal insufficiency.

Preparation

Add 25 g of glacial acetic acid solution containing methyl 1-((dimethylamino)methyl)-4-hydroxy-7-phenoxyisoquinolyl-3-carboxylate into a 1 L four-necked flask which contain 13 g Zinc powder. Then in a stirring state, add 7.5g of 5% dilute hydrochloric acid and raise the temperature to 50-60 ℃. When the raw materials in the liquid phase have basically reacted, reduce the temperature. Filter reaction solution.  Rotary evaporated the filtrate obtain 4-Hydroxy-1-methyl-7-phenoxy-3-isoquinolinecarboxylic acid methyl ester (purity: 96.9%, yield: 87.7%).