反应详情

A mixture of phenyl 5-(1,3-dihydroxy-2-(hydroxymethyl)propan-2-yl)isoxazol-3-ylcarbamate (1 equivalent), 7-(2-morpholin-4-yl-ethoxy)-2-(4-aminophenyl)imidazo[2,1-b]benzothiazole (4) (1 equivalent) and 4-(dimethylamino)pyridine (0.05-0.5 equivalents) in anhydrous THF is stirred at a temperature between rt and 50° C. until the reaction is substantially complete as monitored by LCMS or TLC. The reaction mixture is concentrated under reduced pressure and the residue is purified by either preparative reverse-phase HPLC or silica gel flash chromatography to afford 1-[5-(2-hydroxy-1,1-bis-hydroxymethyl-ethyl)-isoxazol-3-yl]-3-{4-[7-(2-morpholin-4-yl-ethoxy)-benzo[d]imidazo[2,1-b]thiazol-2-yl]-phenyl}-urea (I-1b).

1. concentrationThe reaction mixture is concentrated under reduced pressure
2. customthe residue is purified by either preparative reverse-phase HPLC or silica gel flash chromatography