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1 Wiadomości Chemiczne

1 2002

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Amlodypina, nowoczesny antagonista wapnia - metody syntezy

Hajmowicz H., Jańczewski D., Synoradzki L.

Wiadomości Chemiczne

2002

[Z] 56, 5-6

469-481

The paper is a review of the methods of synthesis of amlodypine, 3-ethyl-5-methyl-2-(2-aminoethoxymethyl)-4-(2-chlorophenyl)-1,4-dihydro-6-methyl-pyridino-3,5-dicarboxylate, a modern drug belonging to the calcium antagonists group. The synthesis of amlodypine is a multistep process. A Williamson reaction with the formation of a compound with an ether bond is usually the first step. This reaction is followed by a Hantzsch reaction with the formation of a correspondingly substituted dihydropyridine ring. Two routes of the realization of this step, which limits the overall process yield, are described. Chlorobenzoic aldehyde and 4-(2-RN-ethoxy) ethyl acetylacetate are substrates in both routs. Nitrogen in the dihydropyridine ring originates either from methyl aminocrotonate (route I) or from ammonium acetate (by amination of 5) (route II). Amlodypine is formed in the third step after deprotecting the amine group or introducing the amine group into the molecule. The formation of amlodypine benzenosulfonate can follow or it can be combined with the third step. There are two valid patents in Poland concerning the preparation of amlodypine benzenosulfonate of Pfizer and of Lek Polska. A patent application of Adamed is under consideration of the Patent Office.