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 Production Method of Lorcainide hydrochloride
  • Production Method of Lorcainide hydrochloride
  • Lorcainide hydrochloride (CAS NO.: ), with its systematic name of acetamide, N-(4-chlorophenyl)-N-(1-(1-methylethyl)-4-piperidinyl)-, monohydrochloride, could be produced through many synthetic methods.

    Following is one of the synthesis routes:

    Production Method of Lorcainide hydrochloride

    Production Method of Lorcainide hydrochloride

    p-Chloroaniline (I) could react with ethyl 4-oxopiperidine-1-carboxylate (II) in the presence of tosyl chloride in refluxing toluene to produce ethyl 4-(p-chlorophenylimino)piperidine-1-carboxylate (III), and then the yielding product could be reduced with NaBH4 in refluxing methanol to produce ethyl 4-(p-chloroanilino)piperidine-1-carboxylate (IV). Next, the acylation of (IV) with phenylacetyl chloride (A) in refluxing benzene affords ethyl 4-[N-(p-chlorophenyl)-N-(phenylacetyl)amino]piperidine-1-carboxylate (V), which is decarboxylated with hot aqueous HBr giving N-(p-chlorophenyl)-N-(piperidin-4-yl)phenylacetamide hydrochloride (VI). At last, this compound is alkylated with 2-bromopropane (B) and Na2CO3 in refluxing butanol.


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