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

Siva Rama Kasibabu Velugula; Nimesh Chandra Misra; Suresh Chapala; Sunil Kumar Reddy Aaramadaka; Ramadas Chavakula; Paul Douglas Sanasi

doi:10.1021/acsomega.2c07305

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

ACS Omega. 2023 Jan 10;8(3):3415-3422. doi: 10.1021/acsomega.2c07305. eCollection 2023 Jan 24.

Authors

Siva Rama Kasibabu Velugula^{1

2}, Nimesh Chandra Misra¹, Suresh Chapala¹, Sunil Kumar Reddy Aaramadaka¹, Ramadas Chavakula¹, Paul Douglas Sanasi²

Affiliations

¹ Chemical Research Department, APL Research Centre-II, Aurobindo Pharma Limited, Indrakaran 502329, Telangana, India.
² Department of Engineering Chemistry, A. U. College of Engineering (A), Andhra University, Visakhapatnam 530003, India.

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%).