Fumaric Acid → (R)-{5-[6-(1-Aza-bicyclo[2.2.2]oct-3-yloxy)-pyridazin-3-yl]-1H-indol-3-ylmethyl}-dimethyl-amine bis(fumarate)

関与物質

反応手順

The product of Example 22A (80 mg, 0.21 mmol) was treated with fumaric acid (Aldrich, 49 mg, 0.42 mmol) in EtOAc/MeOH (v. 10:1) to give the title compound as white solid (74.8 mg, 53%). 1H NMR (MeOH-D4, 300 MHz) 1.79-2.17 (m, 3H), 2.25-2.41 (m, 1H), 2.54-2.61 (m, 1H), 2.84 (s, 6H), 3.19-3.42 (m, 5H), 3.78-3.90 (m, 1H), 4.50 (s, 2H), 5.45-5.54 (m, 1H), 6.66 (s, 5H), 7.34 (d, J=9.2 Hz, 1H), 7.54-7.63 (m, 2H), 7.84 (dd, J=8.5, 1.7 Hz, 1H), 8.17 (d, J=9.2 Hz, 1H), 8.35 (s, 1H) ppm. MS (DCI/NH3) m/z 378(M+H)+. Anal. Calculated for C22H27N5O.2.5 C4H4O4.0.5 H2O: C, 56.80; H, 5.66; N, 10.35. Found: C, 56.62; H, 5.78; N, 10.09.

情報源と証拠