Ethyl isocyanate → [4-(1-Ethylcarbamoyl-piperidin-4-yloxy)-6-fluoro-naphthalen-2-yl]-acetic acid methyl ester

Participants

Reaction Steps

A mixture of [6-fluoro-4-(piperidin-4-yloxy)-naphthalen-2-yl]-acetic acid methyl ester (the intermediate for example 4-1, 1st step, 20 mg, 0.063 mmol) and isocyanato-ethane (0.05 mL) and dichloromethane was stirred at room temperature for 4 hours. The resulting mixture was concentrated in vacuo. The residue was purified by flash column (gradient elution with 0-30% ethyl acetate in petroleum ether) to afford [4-(1-ethylcarbamoyl-piperidin-4-yloxy)-6-fluoro-naphthalen-2-yl]-acetic acid methyl ester (21.0 mg, 85%) as a viscous oil.

Provenance & Evidence