Reaction Steps
A solution of 2-chloro-N-(4′-{[(cyclopropylmethyl)amino]carbonyl}-6-methyl-1,1′-biphenyl-3-yl)isonicotinamide (50 mg, 0.12 mmol) and 2-(methoxymethyl)pyrrolidine (1 ml) in DMSO (1 ml) was heated at 140° C. for 24 h in a sealed tube. The reaction was concentrated under vacuum, the residue chromatographed on an SPE (C18) eluting with a water/acetonitrile gradient, to give, after evaporation of the solvents under vacuum N-(4′-{[(cyclopropylmethyl)amino]carbonyl}-6-methyl-1,1′-biphenyl-3-yl)-2-(2-methoxymethylpyrrolidin-1-yl)isonicotinamide (16 mg). NMR; δH [2H6]—DMSO 10.29,(1H, s), 8.62,(1H, t), 8.21,(1H, d), 7.93,(2H, d), 7.70,(1H, dd), 7.65,(1H, d), 7.44,(2H, d), 7.30,(1H, d), 7.00,(1H, d), 6.89,(1H, s), 4.23,(1H, b), 3.52-3.47,(2H, m), 3.26,(5H, m), 3.16,(2H, t), 2.20,(3H, s), 2.07-1.90,(4H, m), 1.04,(1H, m), 0.43,(2H, m), 0.24,(2H, m). LCMS: retention time 2.78 min, MH+499.
