Development of an Intrinsically Safer Methanolysis/Aromatic Nitro Group Reduction for Step 1 and 2 of Talazoparib Tosylate

Development of an Intrinsically Safer Methanolysis/Aromatic Nitro Group Reduction for Step 1 and 2 of Talazoparib Tosylate

A change in facility for the synthesis of the step 2 intermediate for talazoparib tosylate (1·TsOH) required the development of an alternative, intrinsically safer process. Rapid route scouting and considerations of process safety enabled the development of a telescoped two-step process that was dem...

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Veröffentlicht in:Organic process research & development 2021-12, Vol.25 (12), p.2686-2692
Hauptverfasser: Daniels, David S. B, Crook, Robert, Dirat, Olivier, Fussell, Steven J, Gymer, Adam, Hawksworth, Michael, Knight, Craig J, Laity, Daniel, Mathew, Suju P, Oke, Samantha V, Peach, Philip, Prior, Samantha
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Sprache:eng
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Zusammenfassung:A change in facility for the synthesis of the step 2 intermediate for talazoparib tosylate (1·TsOH) required the development of an alternative, intrinsically safer process. Rapid route scouting and considerations of process safety enabled the development of a telescoped two-step process that was demonstrated on a multikilogram scale.
ISSN:1083-6160
1520-586X
DOI:10.1021/acs.oprd.1c00259