Sodium Methoxide → 2-Piperidinone, 3-amino-3-(difluoromethyl)-

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Reaction Steps

To a solution of methyl-2-difluoromethyl-2,5-diamino-pentanoate-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: (mp: 149° C.) or by distillation (bp: 135° C./0.05 mmHg).

Provenance & Evidence