Hydrochloric Acid → HCID 18186452, compound

Participants

Reaction Steps

4-Anilino-5-(ethoxymethyl)-2-{4-[2-hydroxy-3-(N,N-dimethylamino)propoxy]anilino}pyrimidine (Example 86, 70 mg, 0.16 mmol) was dissolved in formamide (5 ml). Ethereal hydrogen chloride (1.0M; 0.19 ml, 0.19 mmol) was added, and the mixture was heated on power level 2 in a Toshiba Deltawave III domestic microwave oven (650 W) for 90 seconds. Excess formamide was removed by vacuum distillation and the residue was triturated with ethanol and diethyl ether, giving the product as a hygroscopic dihydrochloride salt (20 mg, 24%). NMR: 2.18 (s, 6H), 2.2-2.45 (m, 2H), 3.75-3.9 (m, 3H), 4.21 (d, 2H), 4.76 (br d, 1H), 6.79 (d, 2H), 7.01 (t, 1H), 7.29 (dd, 2H), 7.52 (d, 2H), 7.71 (d, 2H), 7.92 (s, 1H), 8.13 (d, 1H), 8.69 (t, 1H), 8.92 (s, 1H), 8.94 (s, 1H); MS (MH+): 437.4.

Provenance & Evidence