Hydrochloric Acid → HCID 59118111, compound

Participants

Reaction Steps

The product of Example 86 (100 mg, 0.16 mmol), 1-[(3-dimethylamino)propyl]-3-ethylcarbodiimide (36 mg, 0.19 mmol), dimethylaminopyridine (20 mg, 0.16 mmol), and methylsulfonamide (17 mg, 0.18 mmol) were dissolved in 2 mL methylene chloride and stirred overnight at room temperature. The mixture was treated with 0.5 mL 4 M HCl in 1,4-dioxane was added, the solution stirred for 0.5 hours, concentrated to dryness and the residue was purified by preparative HPLC to obtain the title compound (47 mg, 62%). 1H NMR (CD3CN-d3) δ: 8.91 (s, 1 H), 8.76 (d, 1 H), 8.51 (d, 1 H), 8.07 (s, 1 H), 7.97 (t, 1 H), 7.88-7.83 (m, 2 H), 7.62-7.56 (m, 1 H), 7.50-7.47 (m, 2 H), 6.98 (d, 1 H), 5.46 (d, 1 H), 4.54-4.47 (m, 1 H), 3.52 (dd, 2 H), 3.37 (s, 3 H), 3.39-3.25 (m, 2 H), 2.99-2.90 (m, 2 H), 2.14-2.09 (m, 1 H), 1.86-1.79 (m, 1 H). MH+=482.2

Provenance & Evidence