SYNTHESIS OF BENZONITRILES AND BENZIMIDATES

摘要

Benzonitrites and benzimidates represent important intermediates and starting materials, which are typically not commercially available. The present invention discloses a facile synthesis for 2,4-dihydroxybenzonitrile, and ethers and diethers thereof, from 2,4-dihydroxybenzoic acid and from 2,4-dihydroxybenzaldehyde. In addition, the invention discloses a method of preparing substituted benzimidates from substituted benzoic acid. The present invention also discloses a method of preparing a class of iron chelating agents related to desferrithiocin, all of which contain a thiazoline ring. In this method, 2,4-dihydroxybenzonitrile or an alkyl 2,4-dihydroxybenzonitrile or an alkyl 2,4-dihydroxybenzimidate is condensed with (S)-2-methylcysteine.