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1. Highly Efficient Synthesis of HIV NNRTI Doravirine

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   25 Jun 2024 | Contributor(s):: Gauthier, Donald R., Sherry, Benjamin D., Cao, Yang, Journet, Michel, Humphrey, Guy, Itoh, Tetsuji, Tschaen, David M.

   The development of an efficient and robust process for the production of HIV NNRTI doravirine is described. The synthesis features a continuous aldol reaction as part of a de novo synthesis of the key pyridone fragment. Conditions for the continuous flow aldol reaction were derived using...

2. 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....

3. A Concise Flow Synthesis of Efavirenz

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   10 May 2024 | Contributor(s):: Correia, Camille A., Gilmore, Kerry, McQuade, D. Tyler, Seeberger, Peter H.

   Efavirenz is an essential medicine for the treatment of HIV, which is still inaccessible to millions of people worldwide. A novel, semi-continuous process provides rac-Efavirenz with an overall yield of 45 %. This streamlined proof-of-principle synthesis relies on the efficient copper-catalyzed...

4. 7-Step Flow Synthesis of the HIV Integrase Inhibitor Dolutegravir

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   Peer-reviewed journal | 09 Jun 2023 | Contributor(s):: Ziegler, RE, Desai, BKJee, JA, Gupton, BF, Roper, TD, Jamison, TF

   Dolutegravir (DTG), an important active pharmaceutical ingredient (API) used in combination therapy for the treatment of HIV, has been synthesized in continuous flow. By adapting the reported GlaxoSmithKline process chemistry batch route for Cabotegravir, DTG was produced in 4.5h in sequential...