反应详情

A solution of EXAMPLE 22A (5.82 g, 16.394 mmol) in DME (80 mL) was treated with 4-chlorophenylboronic acid (3.089 g, 19.673 mmol), CsF (7.476 g, 49.182 mmol) and (Ph3P)2Pd(OAc)2 (1.228 g, 1.639 mmol), heated to reflux for 4 hours, and filtered. The filtrate was partitioned between aqueous NaHCO3 and ethyl acetate. The aqueous layer was extracted with ethyl acetate and the combined extracts were dried (MgSO4), filtered, and concentrated. The residue was purified by silica gel column chromatography with 15% ethyl acetate/hexane to provide the desired product. MS (ESI) m/e 386, 388 (M+H)+.

1. temperatureheated
2. temperatureto reflux for 4 hours
3. filtrationfiltered
4. customThe filtrate was partitioned between aqueous NaHCO3 and ethyl acetate
5. extractionThe aqueous layer was extracted with ethyl acetate
6. dry with materialthe combined extracts were dried (MgSO4)
7. filtrationfiltered
8. concentrationconcentrated
9. customThe residue was purified by silica gel column chromatography with 15% ethyl acetate/hexane