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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| http://dx.doi.org/10.1021/acsomega.2c07305 | DOI Listing |
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Improved Process for the Preparation of Naloxegol Oxalate, an Opiod Receptor Antagonist.
ACS Omega
January 2023
Department of Engineering Chemistry, A. U. College of Engineering (A), Andhra University, Visakhapatnam 530003, India.
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).
View Article and Find Full Text PDFNaloxegol hydrogen oxalate displaying a hydrogen-bonded layer structure.
Acta Crystallogr E Crystallogr Commun
April 2018
University of Innsbruck, Institute of Pharmacy, Innrain 52, 6020 Innsbruck, Austria.
In the salt (5α,6α)-6-[(2,5,8,11,14,17,20-hepta-oxadocosan-22-yl)-oxy]-3,14-dihy-droxy-17-(prop-2-en-1-yl)-4,5-ep-oxy-morphinan-17-ium hydrogen oxalate, CHNO·CHO the polyether unit of the naloxegol cation adopts the shape of a squashed open letter 'O'. In the crystal, the hydrogen oxalate anions are linked into a chain by O-H⋯O hydrogen bonds. Each naloxegol unit is hydrogen bonded to three hydrogen oxalate ions two O-H⋯O and one N-H⋯O inter-actions.
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