Abstract
A highly efficient synthesis of Erismodegib (LDE225) is described. The chlorine of 2-chloro-5-nitropyridine was displaced by 2,6-dimethylmorpholine and the nitro group reduced to give 3-amino-6-(2’,6'-dimethylmorpholino)pyridine. The Suzuki coupling of methyl 3-bromo-2-methylbenzoate with 4-trifluoromethoxy phenylboronic acid gave methyl-4'-(trifluormethoxy) biphenyl-3-carboxylate. These two fragments were coupled through amide bond formation to give Erismodegib. This synthesis procedure which proceeded in high yield did not require special conditions and is suitable for industrial production.
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