Tetrahydrofuran → Diisopropylethylamine

Participants

Reaction Steps

In analogy to the procedure described in example 59b, 4-chloro-6-[4-(4-fluoro-phenyl)-piperidin-1-yl]-2-methylsulfanyl-pyrimidine-5-carbonitrile (example 57a) was treated with 2,2,2-trifluoroethanolate in tetrahydrofurane at room temperature during 18 hours to yield the 4-phenyl-piperidine in the presence of N-ethyl-diisopropylamine at room temperature during 18 hours to yield 4-[4-(4-fluoro-phenyl)-piperidin-1-yl]-2-methylsulfanyl-6-(2,2,2-trifluoro-ethoxy)-pyrimidine-5-carbonitrile as an amorphous, yellow solid; MS: [M+H]+=427.

Provenance & Evidence