HOAt → HCID 44587862, compound

Participants

Reaction Steps

To a solution of 5-(1-methylpiperidin-4-yloxy)biphenyl-2-ylamine (0.27 mmol, step 58.2) and 2-cyano-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxylic acid (0.33 mmol) in DMF (2 mL) are added EDCI-HCl (0.54 mmol) and HOAt (0.54 mmol) at 0° C. After stirring at the ambient temperature overnight, the reaction mixture is purified by RP-HPLC to give the title compound as a white solid; 1H NMR (CDCl3), δ 0.18-0.21 (2H, m), 0.27-0.30 (2H, m), 0.90-0.94 (2H, m), 1.14-1.25 (2H, m), 1.58-1.78 (5H, m), 1.85-1.92 (2H, m), 2.02-2.06 (2H, m), 2.32 (3H, s), 2.70 (2H, br s), 3.41-3.44 (2H, t), 4.35 (1H, m), 6.89 (1H, d), 6.97 (1H, dd), 7.35-7.37 (2H, m), 7.45-7.52 (3H, m), 7.65 (1H, s), 7.92 (1H, s), 8.06 (1H, d), 8.90 (1H, s).

Provenance & Evidence