反应详情

Prepared from cyclopropanesulfonic acid [14-amino-18-(isoquinolin-1-yloxy)-2,15-dioxo-3,16-diaza-tricyclo[14.3.0.04,6]nonadec-7-ene-4-carbonyl]-amide bis hydrochloride (50 mg, 0.075 mmol, 44 μL (0.25 mmol) of DIPEA and 0.17 mL (0.1 mmol) of tetrahydropyran chloroformate (prepared by treating tetrahydro-pyran-4-ol with phosgene) in DCM as described in the procedure above to give 28 mg (52%) of a white solid. Preparative HPLC condition: YMC XTERRA, S5, 19×100 mm, gradient: 50% B to 100% B, 10 min, hold 2 min, flow rate 25 mL/min. LC-MS (Method A, retention time: 3.13 min), MS m/z 724 (M++1).