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Unexpected dealkylation of Bischler-Napieralski cyclization of 2-(3,4-dimethoxy-2- nitro-phenyl)-N-[2-(3,4-dimethoxyphenyl) ethyl]-N-[(S)-1-phenyl-ethyl] acetamide 3 was reported. The electronic effect of the substituent at 2-position of C ring was also discussed.