反应详情

To a 5 mL microwave vial were added methyl 1-{[1-(3-bromobenzyl)-5-(quinolin-2-ylmethoxy)-1H-benzimidazol-2-yl]methyl}cyclopentanecarboxylate (126 mg, 0.21 mmol), Pd(dppf)Cl2.DCM (18 mg, 0.02 mmol), N-(4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl)methanesulfonamide (192 mg, 0.65 mmol), Na2CO3 (0.3 mL, 2 M) and 1,4-dioxane (2.5 mL). The vial was flushed with N2 then capped and placed in a heating block at 80° C. After 16 h mixture was cooled to RT, transferred to a round-bottomed flask and was concentrated to dryness. The residue was purified using FCC to provide the title compound. MS (ESI): mass calcd. for C39H38N4O5S, 674.82; m/z found, 675.2 [M+H]+.

1. customThe vial was flushed with N2
2. customthen capped
3. customplaced in a heating block at 80° C
4. customtransferred to a round-bottomed flask
5. concentrationwas concentrated to dryness
6. customThe residue was purified