反应详情

温度

120 °C

Aniline (16.8 mL, 184 mmol) is added to a solution of (S)-methyl 2-(methylsulfonyloxy)-2-phenylacetate (I5) (22.4 g, 92.0 mmol) in CH3CN (50 mL). The mixture is heated under MW irradiation at 120° C. for 5 minutes (UPLC-MS monitoring: complete conversion). The resulting crude is partitioned between EtOAc (200 mL) and 1N HCl (200 mL) and the aqueous phase is extracted with EtOAc (3×200 mL). The combined organic layers are dried over Na2SO4, filtered and evaporated under vacuum to obtain 20.3 g of a pale yellow solid (92% yield), which is used in the next step without any additional purification.

1. customThe resulting crude is partitioned between EtOAc (200 mL) and 1N HCl (200 mL)
2. extractionthe aqueous phase is extracted with EtOAc (3×200 mL)
3. dry with materialThe combined organic layers are dried over Na2SO4
4. filtrationfiltered
5. customevaporated under vacuum