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1. Process parameter and kinetic study for the azidation of a zidovudine intermediate with sodium azide in microreactors

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   25 Jun 2024 | Contributor(s):: Jiang, Rongkun, Xue, Xiao, Zhao, Fang, Zhu, Weiping, Shang, Minjing, Su, Yuanhai, Xu, Yufang, Qian, Xuhong

   Zidovudine, i.e., AZT, is an indispensable anti-AIDS drug for highly active antiretroviral therapy. The azidation step is of the most vital importance in the synthetic route of zidovudine. Herein we report the use of microreactors in combination with the simplified azidation system instead of...

2. A Continuous Flow Sulfuryl Chloride-Based Reaction—Synthesis of a Key Intermediate in a New Route toward Emtricitabine and Lamivudine

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   25 Jun 2024 | Contributor(s):: Souza, Juliana M. de, Berton, Mateo, Snead, David R., McQuade, D. Tyler

   We demonstrate a continuous two-step sequence in which sulfenyl chloride is formed, trapped by vinyl acetate, and chlorinated further via a Pummerer rearrangement. These reactions produce a key intermediate in our new approach to the oxathiolane core used to prepare the antiretroviral medicines...

3. Synthesis of Dolutegravir Exploiting Continuous Flow Chemistry

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   10 May 2024 | Contributor(s):: Nqeketo, Sinazo, Watts, Paul

   An efficient continuous flow process for the synthesis of dolutegravir, an active pharmaceutical ingredient (API) for HIV treatment, was investigated. The synthetic procedure starts from a readily available benzyl-protected pyran via six chemical transformations using continuous flow reactors....