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
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container_end_page 1364
container_issue 10
container_start_page 1360
container_title Organic process research & development
container_volume 22
creator Bremberg, Ulf
Eriksson-Bajtner, Johan
Lehmann, Fredrik
Oltner, Viveca
Sölver, Ellen
Wennerberg, Johan
description 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.
doi_str_mv 10.1021/acs.oprd.8b00092
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title Development of a Synthesis of Kinase Inhibitor AKN028
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