反应详情

Prepared from a mixture of 2,4-difluoro-5-sulfobenzoic acid 885-6b (580 mg, 0.58 mmol, 2 equiv), 1-(8-{2-[4-(3-fluorophenyl)-4-piperidinyl]ethyl}-8-azabicyclo[3.2.1]oct-3-yl)-2-methyl-1H-benzimidazole (150 mg, 0.29 mmol, 1 equiv), DIEA (260 μL, 1.45 mmol, 5 equiv) and HATU (110 mg, 0.29 mmol, 1 equiv) following the general procedure for 2,4-dichloro-3-[(4-(3-fluorophenyl)-4-{2-[3-(2-methyl-1H-benzimidazol-1-yl)-8-azabicyclo[3.2.1]oct-8-yl]ethyl}-1-piperidinyl)carbonyl]-N-methylbenzenesulfonamide, example 880. The crude product was purified by prep HPLC (HPLC Method C) to afford 2,4-difluoro-5-[(4-(3-fluorophenyl)-4-{2-[3-(2-methyl-1H-benzimidazol-1-yl)-8-azabicyclo[3.2.1]oct-8-yl]ethyl}-1-piperidinyl)carbonyl]benzenesulfonic acid (example 885) as a white solid (40 mg, 22% yield).

1. customThe crude product was purified by prep HPLC (HPLC Method C)