Exploiting the Physical Properties of Diethanolamine Boronic Esters for Process Improvements in AZD5718

The process development toward synthesizing a diethanolamine (DEA) boronic ester and the subsequent Suzuki–Miyaura coupling (SMC) is disclosed herein. A one-pot lithiation–borylation–transesterification was successfully developed to isolate the DEA boronic ester as a stable crystalline solid and avo...

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Veröffentlicht in:Organic process research & development 2023-03, Vol.27 (3), p.488-495
Hauptverfasser: Henry, Jean-Marc, Milne, David, Perkins, Dave, Hicks, William, Hose, David R. J., Campbell, Andrew D., Mullen, Alexander K., Inglesby, Phillip A., Raw, Steven A., Jones, Martin F.
Format: Artikel
Sprache:eng
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