Seeking for Selectivity and Efficiency: New Approaches in the Synthesis of Raltegravir,Organic Process Research & Development

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Seeking for Selectivity and Efficiency: New Approaches in the Synthesis of Raltegravir
Organic Process Research & Development ( IF 3.1 ) Pub Date : 2020-05-20 , DOI: 10.1021/acs.oprd.0c00155
Francesco Caputo ₁ , Stefano Corbetta ₁ , Oreste Piccolo ₂ , Daniele Vigo ₁

Affiliation

The present work describes the development of an improved synthesis of active pharmaceutical ingredient raltegravir. The isolation of a new process intermediate and the newly developed conditions solve the issue of selectivity typical of this production process, with no need for the use of protecting groups, making the present route more efficient and sustainable than what was reported before. Efficiency comparisons with the previous processes confirm the result here obtained.

中文翻译：

寻求选择性和效率：Raltegravir合成的新方法

本工作描述了活性药物成分raltegravir的改良合成方法的发展。新工艺中间体的分离和新开发的条件解决了该生产工艺典型的选择性问题，而无需使用保护基，这使当前路线比以前报道的更加有效和可持续。与先前过程的效率比较证实了此处获得的结果。

更新日期：2020-06-19

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