Ammonia → HCID 10571424, compound

Participants

Reaction Conditions

Reaction Steps

2-(3-Azidophenyl)benzothiazole (1 g) was added in small portions (5×0.2 g) to a mixture of trifluoromethanesulphonic acid (4 ml), trifluoroacetic acid (5 ml) and triflucromethylacetic anhydride (1 ml) at 0° C. After evolution of nitrogen ceased, the mixture was stirred at 20° C. for 18 hours, basified with aqueous ammonia and the products extracted into ethyl acetate. The organic layer was washed with water, dried (MgSO4) and evaporated to give a gum which was separated on silica with hexane-ethyl acetate (6:4) as eluent. The product obtained was the title compound (70% yield). (Found: M+ 374. C14H9F3N2O3S2 requires MW 374). An in vitro assay of this compound against MCF-7 (wild type) cells gave an IC50 value of 50 nM which again indicates a useful level of activity.

Provenance & Evidence