Improved Process for the Preparation of Naloxegol Oxalate, an Opiod Receptor Antagonist

改进的纳洛昔醇草酸盐(一种阿片受体拮抗剂)制备工艺

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Abstract

The present article discloses an improved and robust commercial process of the modern medicine naloxegol oxalate, which is used to treat opioid-induced constipation. The synthesis originates from the easily available key starting material, viz., naloxone, and ends with the oxalate salt of naloxegol (a pharmaceutically acceptable salt). This novel route has a very high yield and purity greater than 99.5%, substantially free from impurities (less than 1%).

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