Triphenylphosphine → 1-[4-(6-Fluoro-5-octylpyrazin-2-yl)phenoxy]octan-4-yl-dimethylsilane

Participants

Reaction Conditions

Reaction Steps

1.82 ml (11.60 mmol) of diethyl azodicarboxylate are added dropwise at 0° C. to 3.04 g (11.60 mmol) of triphenylphosphine in 85 ml of tetrahydrofuran, and this mixture is stirred at 0° C. for 0.5 hour. 2.00 g (7.00 mmol) of 2-fluoro-3-octyl-6-(4-hydroxyphenyl)-pyrazine (prepared as described in Example 4a to 4d) and 2.46 g (11.60 mmol) of 4-butyldimethylsilylbutanol are subsequently added, and the mixture is stirred at room temperature for 3 hours. The reaction mixture is evaporated, and the residue is purified by chromatography (silica gel/dichloromethane: hexane = 8:2). 1.47 g of 2-fluoro-3-octyl-6-[4-(4-butyldimethylsilylbutyloxy)-phenyl-]pyrazine are obtained. ##STR27##

Provenance & Evidence