An improved and efficient synthesis route to bosutinib is reported. The initial route introduced by Pfizer, implemented Gould-Jacob reactions as key steps. In this protocol, the synthesis, isolation characterization of novel intermediates and their application in the alkylation step for the synthesis of bosutinib are briefly described, using an economic and practical procedure. Ultimately, we provide a new alternative of bosutinib synthesis route, through alkylation of alkali-intermediate with good yield.
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