反应详情

To a solution of 41.6 g diethyl 2-(4-nitro-3-fluorophenyl)-2-methylmalonate III in 210 ml ethyl acetate in a 500-ml Parr hydrogenation bottle is added 830 mg (2 wt %) of 5% palladium/carbon. The mixture is hydrogenated in a Parr apparatus at 25° C. under 10-12 psi hydrogen for 2.5 hours. The catalyst is removed by filtration through diatomaceous earth (Celite®) and is washed with a few ml of ethyl acetate. The solvent is removed in vacuo to give diethyl 2-(4-amino-3-fluorophenyl)-2-methylmalonate as a viscous oil, 37.6 g [100% wt. yield]. This material is used without purification.

1. customThe catalyst is removed by filtration through diatomaceous earth (Celite®)
2. washis washed with a few ml of ethyl acetate
3. customThe solvent is removed in vacuo
4. customto give