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- W4220796272 abstract "Bedaquiline is a crucial medicine in the global fight against tuberculosis, yet its high price places it out of reach for many patients. Herein, we describe improvements to the key industrial lithiation-addition sequence that enable a higher yielding and therefore more economical synthesis of bedaquiline. Prioritization of mechanistic understanding and multi-lab reproducibility led to optimized reaction conditions that feature an unusual base–salt pairing and afford a doubling of the yield of racemic bedaquiline. We anticipate that implementation of these improvements on manufacturing scale will be facile, thereby substantially increasing the accessibility of this essential medication." @default.
- W4220796272 created "2022-04-03" @default.
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- W4220796272 date "2022-03-31" @default.
- W4220796272 modified "2023-10-03" @default.
- W4220796272 title "Diastereoselectivity is in the Details: Minor Changes Yield Major Improvements to the Synthesis of Bedaquiline" @default.
- W4220796272 doi "https://doi.org/10.26434/chemrxiv-2022-cp3g8" @default.
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