反应详情

To a solution of methyl-2-difluoromethyl-2,5-diaminopentanoate-dihydrochloride (2.7 g) in dry methanol (30 ml) is added under nitrogen 2 equivalents of sodium methylate in methanol (0.46 g of sodium in 20 ml of methanol). The reaction mixture is stirred for 3 hours at room temperature then the solvent is evaporated under reduced pressure. The residue is extracted with ether to yield crude 3-amino-3-difluoromethyl-2-piperidone which is purified either by crystallization from CHCl3 /pentane: (m.p.: 149° C.) or by distillation (b.p. 135° C./0.05 mmHg).

1. customthe solvent is evaporated under reduced pressure
2. extractionThe residue is extracted with ether