反应详情

Using the procedure for step D in Example 1, the title compound was prepared from 3-(5-bromo-1H-benzimidazol-2-yl)-1-oxa-2-aza-spiro[4.5]dec-2-ene (150 mg, 0.449 mmol, as prepared in the previous step) and 3,3-dimethyl-3H-benzo[c][1,2]oxaborol-1-ol (2.0 eq., 145 mg, 0.898 mmol, prepared as described in US2007/259936) and (dppf)PdCl2.DCM (0.10 eq., 36.6 mg, 0.045 mmol) in 9% yield (16.4 mg). 1H-NMR (400 MHz, d4-MeOH) δ: 7.82 (dd, J=8.1, 1.3 Hz, 1H), 7.53-7.68 (m, 1H), 7.47 (br. s., 1H), 7.35 (td, J=7.6, 1.6 Hz, 1H), 7.19-7.24 (m, 2H), 7.05 (dd, J=7.6, 1.3 Hz, 1H), 3.28 (s, 2H), 1.69-1.90 (m, 6H), 1.46-1.65 (m, 4H), 1.33 (s, 6H). Mass Spectrum (LCMS, ESI pos.): Calcd. for C24H27N3O2: 390.2 (M+H). found: 390.4.