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Highly Efficient Synthesis of Dolutegravir

  • Dong Yan,
  • Xixi Hou,
  • Ziyuan Wu,
  • Xinyan Wang,
  • Xueqin Hao,
  • Lan Wang,
  • Longfei Mao

摘要

Abstract

Dolutegravir, a potent HIV integrase inhibitor, is currently synthesized via routes that have several drawbacks, including low yields, high formation of by-products, and complexities of operations. In this study, we seek to tackle these challenges by developing a new synthesis route for dolutegravir. We designed a new synthesis route based on the existing one, utilizing low-cost starting materials to achieve a dolutegravir production purity of 99.6%. We thus overcome the limitations of the existing synthesis methods and improve the overall efficiency and cost-effectiveness of dolutegravir synthesis.