反应详情

1-[(2,2-Difluorocyclopropyl)methyl]-3-methyl-5-(octahydrocyclopenta[c]-pyrrol-5-yl)-1,3-dihydro[1,2,5]thiadiazolo[3,4-b]pyridine 2,2-dioxide (25-1, 20 mg, 0.052 mmol, 1.0 equiv), (2R)-2-hydroxypropanoic acid (25-2, 7.0 mg, 0.078 mmol, 1.5 equiv), DIPEA (27 μL, 0.16 mmol, 3.0 equiv) and HATU (29.7 mg, 0.078 mmol, 1.5 equiv) were added to anhydrous acetonitrile (520 μL). After stirring for 10 min at room temperature, LCMS showed consumption of starting material. Purification by reverse-phase HPLC (20-100% CH3CN:0.1% TFA in H2O) provided 25-3 as a white solid. MS m/z (M+H): calculated=457.1716; observed=457.1726.

1. customconsumption of starting material
2. customPurification by reverse-phase HPLC (20-100% CH3CN:0.1% TFA in H2O)