Hydrochloric Acid → 2-[(3-{4-[(benzyl{2-methyl-3-[(methylsulfonyl)amino]phenyl}amino)methyl]phenoxy}phenoxy)methyl]cyclopropanecarboxylic Acid

Participants

Reaction Steps

To the product from Example 284A was added 2N hydrochloric acid (1 mL), tetrahydrofuran (0.5 mL) and water (0.5 mL). The reaction mixture was stirred at room temperature overnight. Water (2 mL) was added. The solution was neutralized with 1N hydrochloric aid until pH=2˜3. The product was extracted with ethyl acetate (2 mL), dried in vaccuo, and purified by HPLC to provide the titled compound. 1H NMR (500 MHz, DMSO-d6) δ12.01-12.29 (br.s, 1 H), 8.95 (s, 1 H), 7.23 (m, 8 H), 7.03 (m, 1 H), 6.94 (m, 4 H), 6.69 (m, 1 H), 6.50 (m, 2 H), 4.06 (s, 2 H), 4.03 (s, 2 H), 3.94 (m, 1 H), 3.80 (m, 1 H), 2.91 (s, 3 H), 2.40 (s, 3 H), 1.67 (m, 1 H), 1.57 (m, 1 H), 1.05 (m, 1 H), 0.92 (m, 1 H); MS (APCI+) m/z 587.1 (M+H)+.

Provenance & Evidence