Triethylamine → 6-(2-Amino-pyrimidin-4-yloxy)-benzo[d]isothiazole-3-carboxylic acid (4-fluoro-3-trifluoromethyl-phenyl)-amide

Participants

Reaction Steps

Hydrogenation of 51 mg (0.11 mMol) of 6-(2-amino-6-chloro-pyrimidin-4-yloxy)-benzo[d]isothiazole-3-carboxylic acid (4-fluoro-3-trifluoromethyl-phenyl)-amide (Step 6.3) in 10 ml THF and 46 μl (0.33 mMol) Et3N in presence of two portions of 0.1 g Pd/C (10%; Engelhard 4505) during 36 h, filtration, concentration of the filtrate and chromatography (Combi Flash; CH2Cl2/hexane 2:3→CH2Cl2→CH2Cl2/ether 7:3) gives the title compound: m.p.: 237-239° C.; MS: [M+1]+=450.

Provenance & Evidence