反应详情

1-(tert-butoxycarbonyl)indoline-7-carboxylic acid (300 mg, 1.14 mmol), HATU (475 mg, 21.2 mmol) and methyl 4-(1-aminocyclopropyl)benzoate (262 mg, 1.37 mmol) were added to acetonitrile (7.6 ml). The solution was cooled in an ice bath and DIPEA (695 ul, 3.99 mmol) was added. After 2 hr at RT, the mixture was poured into a solution of NaHCO3 (½ sat.) and washed 3 times with EtOAc. The combined organic layers were washed with brine and dried with Na2SO4. The solvent was removed and the crude mixture purified by flash chromatography on silica gel. The Boc group was removed with 1:1 TFA/DCM using the standard procedure.

1. temperatureThe solution was cooled in an ice bath
2. washwashed 3 times with EtOAc
3. washThe combined organic layers were washed with brine
4. dry with materialdried with Na2SO4
5. customThe solvent was removed
6. customthe crude mixture purified by flash chromatography on silica gel
7. customThe Boc group was removed with 1:1 TFA/DCM using the standard procedure