Potassium Iodide → 5-(4-Methanesulfonyl-phenyl)-2-{1-[(1-trifluoromethyl-cyclopropyl)methyl]-piperidin-4-yl}-2,3-dihydro-furo[2,3-c]pyridine

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Reaction Conditions

Reaction Steps

A mixture of 5-(4-methanesulfonyl-phenyl)-2-piperidin-4-yl-2,3-dihydro-furo[2,3-c]pyridine (435 mg), methanesulfonic acid (1-trifluoromethyl-cyclopropyl)methyl ester (700 mg), potassium carbonate (850 mg), and potassium iodide (100 mg) in N-methyl-2-pyrrolidone (8 mL) is stirred at 100° C. for 4 h and then at room temperature overnight. The solvent is evaporated and the residue is triturated with methanol and filtered. The filtrate is concentrated in vacuo and the residue is purified by HPLC to give the title compound. LC (method 1): tR=1.09 min; Mass spectrum (ESI+): m/z=481 [M+H]+.

Provenance & Evidence