Methyl 3-aminocrotonate → Palonidipine

Participants

Reaction Steps

To a solution of a mixture 290 mg of 3-(N-benzyl-N-methylamino)-2,2-diethylpropyl acetoacetate and 15 mg of methyl 3-aminocrotonate in 1 ml of 2-propanol was added 168 mg of 2-fluoro-5-nitrobenzaldehyde. The mixture was refluxed for 10 hours. The solvent was distilled off to leave the residue. The residue was purified by a column chromatography (n-hexane:ethyl acetate=2:1) on silica gel to provide 184 mg (yield 34%) of the desirec compound (140).

Provenance & Evidence