N-Substd. 2-imino-benzothiazoline prodn. - from the unsubstd. deriv. and amine in presence of acidic catalyst

摘要

Prodn. of N-substd. 2-iminobenzothiazolines of formula (I) is effected by reacting 2-iminobenzothiazoline of formula (II) with an amine of formula R2NH2 (III) in the presence of an acid catalyst. In formulae, R1=alkyl, R2=opt. substd. alkyl or benzyl; and Rn= H, alkyl gps., halogen atoms, NO2, alkoxy or alkanoyl gps. or a CN gp. The reaction is effected at 100-200 deg.C in an inert organic solvent in the presence of 5-50 mole.% p-toluenesulphonic acid (TsOH). The (III):(II) molar ratio is 10-30:1. USE/ADVANTAGE - (I) are useful as intermediates, e.g. for pharmaceuticals. The process is simple and gives high yields (e.g. 91-99%) of high purity (I).