反应详情

Add Pd(OAc)2 (15 mg, 0.07 mmol) and Ph3P (47 mg, 0.18 mmol) to a stirred solution of trifluoro-methanesulfonic acid 6-methoxy-1-[4-(2-piperidin-1-yl-ethoxy)-benzoyl]-naphthalen-2-yl ester (600 mg, 1.1 mmol) in DME at r.t. Add Na2CO3 solution (2 mL of 2 M) followed by 1-hydroxy-2,1-benzoxaborolane (200 mg, 1.5 mmol). Stir at r.t. for 2 h and heat gently (˜50° C.) for 6 h. Dilute with CH2Cl2 and wash with water and brine, dry over MgSO4, filter and concentrate. Purify the crude product by flash chromatography (0-5% (2M NH3 in MeOH)/CH2Cl2 to yield [2-(2-hydroxymethyl-phenyl)-6-methoxy-naphthalen-1-yl]-[4-(2-piperidin-1-yl-ethoxy)-phenyl]-methanone (171 mg, 31%).

1. temperatureheat gently (˜50° C.) for 6 h
2. washwash with water and brine
3. dry with materialdry over MgSO4
4. filtrationfilter
5. concentrationconcentrate
6. customPurify the crude product by flash chromatography (0-5% (2M NH3 in MeOH)/CH2Cl2