OSD
Ulf Bremberg, Johan Eriksson-Bajtner, Fredrik Lehmann, Viveca Oltner, Ellen Sölver, and Johan Wennerberg
Org. Process Res. Dev. 2018, 22, 1360−1364
ABSTRACT: 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.
Keywords
tyrosine kinase inhibitor, SNAr reaction, Suzuki coupling, removal of palladium