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Improved Process for the Preparation of Naloxegol Oxalate, an Opiod Receptor Antagonist
ACS Omega ( IF 3.7 ) Pub Date : 2023-01-10 , DOI: 10.1021/acsomega.2c07305 Siva Rama Kasibabu Velugula 1, 2 , Nimesh Chandra Misra 1 , Suresh Chapala 1 , Sunil Kumar Reddy Aaramadaka 1 , Ramadas Chavakula 1 , Paul Douglas Sanasi 2
ACS Omega ( IF 3.7 ) Pub Date : 2023-01-10 , DOI: 10.1021/acsomega.2c07305 Siva Rama Kasibabu Velugula 1, 2 , Nimesh Chandra Misra 1 , Suresh Chapala 1 , Sunil Kumar Reddy Aaramadaka 1 , Ramadas Chavakula 1 , Paul Douglas Sanasi 2
Affiliation
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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%).
中文翻译:
阿片受体拮抗剂草酸纳洛昔康的制备工艺改进
本文公开了现代药物纳洛昔康草酸盐的改进且稳健的商业化工艺,用于治疗阿片类药物引起的便秘。合成源自容易获得的关键原料,即纳洛酮,并以纳洛昔康的草酸盐(药学上可接受的盐)结束。这条新路线具有非常高的产率和大于 99.5% 的纯度,基本上不含杂质(小于 1%)。
更新日期:2023-01-10
中文翻译:
![](https://scdn.x-mol.com/jcss/images/paperTranslation.png)
阿片受体拮抗剂草酸纳洛昔康的制备工艺改进
本文公开了现代药物纳洛昔康草酸盐的改进且稳健的商业化工艺,用于治疗阿片类药物引起的便秘。合成源自容易获得的关键原料,即纳洛酮,并以纳洛昔康的草酸盐(药学上可接受的盐)结束。这条新路线具有非常高的产率和大于 99.5% 的纯度,基本上不含杂质(小于 1%)。