An alternative and highly efficient synthetic protocol of Osimertinib

Osimertinib, a third generation potent and specific EGFR inhibitor is an
important drug against many forms of cancer. It was synthesized by an
improved and highly efficient protocol, revisiting the classical synthetic
process and modifying parameters, such as solvents, temperature, reagents,
and reaction time. A cost-effective, environmentally friendly methodology
for the synthesis of Osimertinib was established, which gave shorter
reaction times, saved labor by eliminating purification steps through
column chromatography, and enhanced yields. Four of the seven steps in
total, were proceeded quantitatively or almost quantitatively (~ 98%).
This synthetic protocol provides a very high overall yield, up to 68%. In
addition, the entire approach enables the preparation of Osimertinib
analogues and could be extended in the synthesis of other structurally
similar bioactive compounds.