反应详情

A solution of methanesulfonyloxy-(5-methyl-thiophen-2-yl)-acetic acid methyl ester (I266) (2.10 g, 7.94 mmol), aniline (1.09 mL, 11.9 mmol) and N-ethyl-N-isopropylpropan-2-amine (2.04 mL, 11.9 mmol) in MeCN (10 mL) is heated under microwave irradiation at 100° C. for 1 hour. The solvent is removed, DCM is added and the organic phase is washed with water and brine, dried over Na2SO4 and evaporated. The resulting brown oil is purified by silica gel flash chromatography (Hexane/EtOAc=9575 to 90/10) to obtain intermediate I269 as a yellow oil (500 mg, 24% yield).

1. customThe solvent is removed
2. additionDCM is added
3. washthe organic phase is washed with water and brine
4. dry with materialdried over Na2SO4
5. customevaporated
6. customThe resulting brown oil is purified by silica gel flash chromatography (Hexane/EtOAc=9575 to 90/10)