DAI Liyan, YUAN Gengyang, YU Yifu, et al. Improved synthetic process for 3-benzyloxy-4-n-butylaniline hydrochloride[J]. CIESC Journal, 2010, (12): 3130-3134.
DAI Liyan, YUAN Gengyang, YU Yifu, et al. Improved synthetic process for 3-benzyloxy-4-n-butylaniline hydrochloride[J]. CIESC Journal, 2010, (12): 3130-3134.DOI:
An improved synthetic process for 3-benzyloxy-4-n-butylaniline hydrochloride the key intermediate of nequinate which is an anticoccidal drug to parasites of Eimeria
was described.The process was started with 3-aminophenol
via acylation
Fries rearrangement
benzylation
hydrolysis
and Huang-Minlon reduction
to give the title compound.The optimal reaction conditions and molar yield were as follows: acylation
130—140℃ for 3 h; Fries rearrangement
140℃ for 5 h
77.9%(based on 3-aminophenol); benzylation
70℃ for 2 h and 80℃ for 4 h
81.3%; hydrolysis and Huang-Minlon reduction
reflux for 90 min
78.2%.The structures of the main compounds were confirmed by 1H NMR. The process is much of industrial value because of high yields
cheap and available materials
moderate reaction conditions and convenient operations.