American Chemical Society
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Highly Efficient Synthesis of HIV NNRTI Doravirine

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journal contribution
posted on 2015-03-20, 00:00 authored by Donald R. Gauthier, Benjamin D. Sherry, Yang Cao, Michel Journet, Guy Humphrey, Tetsuji Itoh, Ian Mangion, David M. Tschaen
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 microbatch snapshots of the flow process.