4-Amino-3-ethoxy-5-ethoxycarbonylisothiazole-1,1-dioxide → ethyl 4-amino-3-[[2-hydroxy-3-[[3-(piperidin-1-ylmethyl)phenyl]methoxy]propyl]amino]-1,1-dioxo-1,2-thiazole-5-carboxylate

Participants

Reaction Steps

1.39 g (5 mmol) of 2-hydroxy-3-[3-(1-piperidylmethyl)benzyloxy]propylamine are added dropwise to a suspension of 1.24 g (5 mmol) of 4-amino-3-ethoxy-5-ethoxycarbonylisothiazole-1,1-dioxide in 10 ml of acetonitrile and the mixture is stirred for 5 hours at room temperature. The residue obtained after evaporation of the solvent under vacuum is chromatographed with methanol against silica gel. The main fraction yields 2.06 g (86%) of the title compound.

Provenance & Evidence