Development of a Synthesis of Kinase Inhibitor AKN028

Development of a Synthesis of Kinase Inhibitor AKN028

The novel tyrosine kinase inhibitor AKN028 has demonstrated promising results in preclinical trials. An expedient protocol for the synthesis of the compound at kilogram scale is described, including an SNAr reaction with high regioselectivity and a Suzuki coupling. Furthermore, an efficient method f...

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Veröffentlicht in:Organic process research & development 2018-10, Vol.22 (10), p.1360-1364
Hauptverfasser: Bremberg, Ulf, Eriksson-Bajtner, Johan, Lehmann, Fredrik, Oltner, Viveca, Sölver, Ellen, Wennerberg, Johan
Format: Artikel
Sprache:eng
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Zusammenfassung:The novel tyrosine kinase inhibitor AKN028 has demonstrated promising results in preclinical trials. An expedient protocol for the synthesis of the compound at kilogram scale is described, including an SNAr reaction with high regioselectivity and a Suzuki coupling. Furthermore, an efficient method for purification and removal of residual palladium is described.
ISSN:1083-6160
1520-586X
DOI:10.1021/acs.oprd.8b00092