Yan Xi-long
2004
Citations
0
Influential Citations
4
Citations
Journal
Fine chemicals
Abstract
Ethambutol is the key intermediate of ethambutol hydrochloride which is used as a chiral antituberculosis agent.(R,S)-2-Aminobutanol was synthesized from 1-butene,chlorine and acetonitrile in a yield of 50.7%.Resolution of (R,S)-2-aminobutanol with L-(+)-tartaric acid gave(S)-2-aminobutanol L-(+)-tartrate in 94.3% yield,and (R)-2-aminobutanol L-(+)-tartrate was produced in 99.0% yield after the treatment of the filtrate.The optically pure (S)-2-aminobutanol and (R)-2-aminobutanol were both obtained in over 85.0% yield after the hydrolysis of (S)- and (R)-2-aminobutanol L-(+)-tartrate separately.Finally,ethambutol was obtained in 81.3% yield from (S)-2-aminobutanol and 1,2-dichloroethane.Furthermore,racemization of (R)-2-aminobutanol using Raney Ni as catalyst afforded (R,S)-2-aminobutanol in a yield of 72.7%.L-(+)-Tartaric acid was recovered in a yield of 82.5% from sodium tartrate which was obtained through the hydrolysis of 2-aminobutanol L-(+)-tartrate.