Ethanolamine → 4-[4-(4-Fluoro-phenyl)-piperidin-1-yl]-2-(2-hydroxy-ethylamino)-6-(2,2,2-trifluoro-ethoxy)-pyrimidine-5-carbonitrile

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Reaction Steps

In analogy to the procedure described in example 57c, 4-[4-(4-fluoro-phenyl)-piperidin-1-yl]-2-methylsulfanyl-6-(2,2,2-trifluoro-ethoxy)-pyrimidine-5-carbonitrile (example 61a) was oxidized by 3-chloro-perbenzoic acid to the 4-[4-(4-fluoro-phenyl)-piperidin-1-yl]-2-methanesulfonyl-6-(2,2,2-trifluoro-ethoxy)-pyrimidine-5-carbonitrile which was then treated with ethanolamine in dioxane at 40° C. during 4 hours to yield 4-[4-(4-fluoro-phenyl)-piperidin-1-yl]-2-(2-hydroxy-ethylamino)-6-(2,2,2-trifluoro-ethoxy)-pyrimidine-5-carbonitrile as a clorless oil; MS: [M+H]+=440.

Provenance & Evidence