| 摘要 |
Benzyl sulphinyl benzimidazoles of formula (I) are new. R1 = H, 1-8C alkyl, cycloalkyl, phenyl or aralkyl R2 = H, or 1-8C alkyl or R1 and R2 together with the N atom form a ring, R3 and R4 = H, halogen, CF3, lower alkyl, lower alkoxy, lower alkoxy carbonyl, or amino. The following process is claimed : a 2-mercapto benzimidazole (II) is condensed with a 2-amino benzyl cpd. (III) and the resultant sulphide (IV) is oxidised, where X is a reactive gp. such as halogen or a sulphonyloxy gp. The first stage is effected in an inert solvent such as toluene, benzene, ethanol or acetate, pref. in the presence of an alkali. Oxidn. may be effected with an organic peracid, hydrogen peroxide, sodium hypochlorite or sodium metaperiodate, pref. at -15 to +5 deg.C in an inert solvent. |
