Ethylene Oxide → (+/-)-2-(3,3-Difluoro-4-{3-methoxy-4-[7-(2-methoxy-pyridin-3-yl)-pyrrolo[2,1-f][1,2,4]triazin-2-ylamino]-phenyl}-piperidin-1-yl)-ethanol

Participants

Reaction Steps

Ethylene oxide and (±)-[4-(3,3-difluoro-piperidin-4-yl)-2-methoxy-phenyl]-[7-(2-methoxy-pyridin-3-yl)-pyrrolo[2,1-f][1,2,4]triazin-2-yl]-amine (Example 12, 68 mg) were converted to the title product by a procedure similar to the one described for Example 8 to give a yellow foam (51 mg, 68% yield). 1H NMR (CDCl3): 8.72 (s, 1H), 8.48 (d, J=7.4 Hz, 1H), 8.28 (d, J=8.1 Hz, 1H), 8.24 (d, J=4.3 Hz, 1H), 7.51 (s, 1H), 7.14 (d, J=3.6 Hz, 1H), 7.08 (m, 1H), 6.84 (m, 2H), 4.02 (s, 3H), 3.92 (s, 3H), 3.68 (m, 2H), 3.25 (m, 1H), 3.10 (m, 1H), 2.90 (m, 1H), 2.74 (m, 1H), 2.65 (m, 1H), 2.46 (dd, J=28.3 (F-H vic. coupling), 11.7 Hz, 1H), 2.27 (m, 3H), 1.90 (m, 1H); LC/MS (ESI+): 510.54 (M+H).

Provenance & Evidence