Amlodipine → (2S)-2-aminobutanedioate;3-O-ethyl 5-O-methyl 2-(2-aminoethoxymethyl)-4-(2-chlorophenyl)-6-methyl-1,4-dihydropyridine-3,5-dicarboxylate

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Reaction Steps

16 g of amlodipine and 12 g of amlodipine maleate were melted in a 300 ml flask. The melted substance was cooled to room temperature and dissolved in 300 ml of dichloromethane. The mixture was extracted with 300 ml of a 1M NaOH solution. The organic layer was discarded and the aqueous layer acidified with 55 ml of a 6 M HCl solution. The mixture was extracted with 300 ml of dichloromethane. The layers were separated and the organic layer dried over Na2SO4. The mixture was evaporated to dryness and the remaining solid recrystallised from ethanol. The obtained solid was dried in a vacuum oven at 40° C. leaving 4.7 g of an off white product.

Provenance & Evidence