Benzoyl isothiocyanate → 1-Benzoyl-3-[3-iodo-5-methoxy-2-(tetrahydro-pyran-4-yl)-pyridin-4-yl]-thiourea

Participants

Reaction Steps

To a stirred solution of 725 mg (2.17 mmol) 3-iodo-5-methoxy-2-(tetrahydro-pyran-4-yl)-pyridin-4-ylamine in 14 ml acetone was added dropwise 0.35 ml (2.60 mmol) benzoyl isothiocyanate at room temperature. The reaction mixture then heated at reflux for 2 h before being cooled to room temperature concentrated in vacuo. Flash chromatography (ethyl acetate/heptane) afforded 868 mg (80%) 1-benzoyl-3-[3-iodo-5-methoxy-2-(tetrahydro-pyran-4-yl)-pyridin-4-yl]-thiourea as a white crystalline solid. ES-MS m/e (%): 498 (M+H+, 100).

Provenance & Evidence