Methanesulfonic Acid → Tirbanibulin Mesylate

Participants

Reaction Steps

2-(5-(4-(2-morpholinoethoxy)phenyl)pyridin-2-yl)-N-benzylacetamide mesylate (KX2-391.MSA) was synthesized in four linear steps starting from compound 5. The first three steps were carried out similar to the procedure discussed above for KX2-391.2HCl to afford methyl 2-(5-(4-(2-morpholinoethoxy)phenyl)pyridin-2-yl)acetate (KX2-391). KX2-391 was converted to the methanesulfonate salt by treatment with methanesulfonic acid (MSA) in acetone at 50° C. to afford 2-(5-(4-(2-morpholinoethoxy)phenyl)pyridin-2-yl)-N-benzylacetamide mesylate (KX2-391.MSA).

Provenance & Evidence