[NH2:1][C:2]1[CH:3]=[CH:4][C:5](Br)=[C:6]2[C:10]=1[C:9](=[O:11])[NH:8][CH2:7]2.CB1OB(C)OB(C)O1.C(=O)([O-])[O-].[K+].[K+].NC1C=CC(C)=C2C=1C(=O)NC2>C(COC)OC.O>[NH2:1][C:2]1[CH:3]=[CH:4][CH:5]=[C:6]2[C:10]=1[C:9](=[O:11])[NH:8][CH2:7]2
In a similar manner to Step 1 of Example 152, 7-amino-4-bromoisoindolinone (100 mg, 0.440 mmol) was dissolved in dimethoxyethane (5 mL), and the solution was treated with trimethylboroxine (0.184 mL, 1.76 mmol), [bis(diphenylphosphino)ferrocene]dichloropalladium (28.7 mg, 0.0352 mmol), potassium carbonate (304 mg, 2.20 mmol) and water (0.158 mL), followed by purification by preparative thin-layer chromatography (chloroform/acetonitrile=4/1) to obtain a mixture of 7-amino-4-methylisoindolinone and 7-aminoisoindolinone (62.9 mg, ratio 10/1, yield 89%).
Wird geladen…
