反应详情

To a stirred solution of (2R)-4-[4-{4-[difluoro(trans-4-hydroxycyclohexyl)methoxy]phenyl}-2-oxopyridin-1(2H)-yl]-2-methyl-2-(methylsulfonyl)-N-(tetrahydro-2H-pyran-2-yloxy)butanamide (280 mg, 0.473 mM) in 2.3 mL of dichloromethane was added a solution of 4 M HCl in dioxane (0.120 mL, 0.473 mM). The reaction mixture was allowed to stir for 20 minutes before being treated with 0.5 mL of MeOH. Reaction was concentrated in vacuo and purified by reverse phase (Shimadzu) prep HPLC 35 mg, (14%). LCMS 529.1 1H NMR (400 MHz, METHANOL-d4) δ ppm 1.30 (br. s., 2 H) 1.40-1.54 (m, 2 H) 1.64-1.74 (m, 3 H) 1.99-2.14 (m, 4 H) 2.31-2.42 (m, 1 H) 2.51-2.67 (m, 1 H) 3.09 (s, 3 H) 3.45-3.62 (m, 1 H) 3.87-4.02 (m, 1 H) 4.23-4.34 (m, 1 H) 6.70-6.75 (m, 1 H) 6.78 (s, 1 H) 7.21-7.33 (m, 2 H) 7.65-7.74 (m, 3 H)

1. customReaction
2. concentrationwas concentrated in vacuo
3. custompurified by reverse phase (Shimadzu)