反应详情

To a suspension of 0.01 g 2-(4-methoxy-7-morpholin-4-yl-benzothiazol-2-yl)-4,5,6,7-tetrahydro-1H-imidazo[4,5-c]pyridine hydrochloride in 0.8 ml tetrahydrofurane were added at 0–4° C. 0.02 ml N-ethyldiisopropylamine and 0.004 ml o-toluoyl chloride. The mixture was refluxed over night, silicagel was added and the solvent was distilled off. The residue was transferred to a column prefilled with silicagel and was chromatographed with ethylacetate/methanol 98:2 to yield 0.006 g (50%)[2-(4-methoxy-7-morpholin-4-yl-benzothiazol-2-yl)-1,4,6,7-tetrahydro-imidazo[4,5-c]pyridin-5-yl]-o-tolyl-methanone as yellow solid; MS (ISP): m/e=490 (M+H+).

1. additionwere added at 0–4° C
2. temperatureThe mixture was refluxed over night
3. additionsilicagel was added
4. distillationthe solvent was distilled off
5. customwas chromatographed with ethylacetate/methanol 98:2