2-氯-6-苯氧基苄胺

反应条件: temp:0.00; pressure:0.00; stir:

反应条件: temp:0.00; pressure:0.00; stir:

反应条件: temp:0.00; pressure:0.00; stir:; See reaction.notes.procedure_details.

实验步骤: 83 mg of the title compound was prepared from 4,5,6,7-tetrahydro-1H-benzimidazole-5-carboxylic acid and 2-chloro-6-phenoxybenzylamine by a similar procedure as described in Example 1.

反应条件: temp:0.00; pressure:0.00; stir:; See reaction.notes.procedure_details.

实验步骤: 83 mg of the title compound was prepared from 4,5,6,7-tetrahydro-1H-benzimidazole-5-carboxylic acid and 2-chloro-6-phenoxybenzylamine by a similar procedure as described in Example 1.

反应条件: temp:0.00; pressure:0.00; stir:; See reaction.notes.procedure_details.

实验步骤: A mixture 6-bromo-4-chloro-2H-phthalazin-1-one (150 mg, 0.58 mmol), 2-chloro-6-phenoxy-benzylamine (150 mg, 0.64 mmol), Pd2(dba)3 (53 mg, 0.058 mmol), rac-BINAP (132 mg, 0.17 mmol) and NaOt-Bu (140 mg, 1.45 mmol) in DMA (6 mL) was heated at 80° C. for 1 h. The mixture was allowed to cool, diluted with EtOAc (25 mL) and washed with water (25 mL). The organic layer was dried over anhydrous sodium sulfate and concentrated. Chromatography on silica (EtOAc/hexanes) yielded the title compound. 4-Chloro-6-(2-chloro-6-phenoxy-benzylamino)-2H-phthalazin-1-one: 39 mg (16.3%): m/z (M+H)=412. 1H-NMR (DMSO-d6) δ: 12.34 (s, 1H), 7.90 (d, 1H), 7.35 (m, 5H), 7.21 (dd, 1H), 7.15 (m, 1H), 7.02 (m, 2H), 6.95 (d, 1H), 6.84 (dd, 1H), 4.50 (d, 2H). to cool washed with water (25 mL) The organic layer was dried over anhydrous sodium sulfate concentrated

反应条件: temp:0.00; pressure:0.00; stir:; See reaction.notes.procedure_details.

实验步骤: A mixture 6-bromo-4-chloro-2H-phthalazin-1-one (150 mg, 0.58 mmol), 2-chloro-6-phenoxy-benzylamine (150 mg, 0.64 mmol), Pd2(dba)3 (53 mg, 0.058 mmol), rac-BINAP (132 mg, 0.17 mmol) and NaOt-Bu (140 mg, 1.45 mmol) in DMA (6 mL) was heated at 80° C. for 1 h. The mixture was allowed to cool, diluted with EtOAc (25 mL) and washed with water (25 mL). The organic layer was dried over anhydrous sodium sulfate and concentrated. Chromatography on silica (EtOAc/hexanes) yielded the title compound. 4-Chloro-6-(2-chloro-6-phenoxy-benzylamino)-2H-phthalazin-1-one: 39 mg (16.3%): m/z (M+H)=412. 1H-NMR (DMSO-d6) δ: 12.34 (s, 1H), 7.90 (d, 1H), 7.35 (m, 5H), 7.21 (dd, 1H), 7.15 (m, 1H), 7.02 (m, 2H), 6.95 (d, 1H), 6.84 (dd, 1H), 4.50 (d, 2H). to cool washed with water (25 mL) The organic layer was dried over anhydrous sodium sulfate concentrated