反应详情

5.3 g (0.027 mol) 2-aminomethyl-8-methoxychroman from example 93 g, 9.5 g (0.03 mol) N-(4-bromobutyl)saccharin, 3.05 g (0.03 mol) triethylamine and 80 ml dimethyl formamide were heated to 50 ° C. for 4 h. work-up as described in example 93h furnished 16.6 g crude product, which was filtered through 175 g silica with toluene/ethyl acetate. This gave 3.4 g dialkylation product and 7.1 g monoalkylation product. Rechromatography of the monoalkylation product on 230 g silica with toluene/methanol (10:1) gave 2.5 g pure 2-{N-[4-(1,1-dioxido-3-oxo-2,3-dihydro-benzisothiazol-2-yl)butyl]aminomethyl}-8-methoxy-chroman.

1. customwere heated to 50 ° C. for 4 h.
2. customfurnished 16.6 g crude product, which
3. filtrationwas filtered through 175 g silica with toluene/ethyl acetate