2-Methyl-3-butyn-2-ol → 4-[1-(2-aminopyrimidin-4-yl)-3-(morpholin-4-ylmethyl)-1H-indazol-6-yl]-2-(1,3-thiazol-2-yl)but-3-yn-2-ol

Participants

Reaction Steps

The title compound was prepared by the procedure described in Example 6-c by substituting 4-{6-bromo-3-[(dimethylamino)methyl]-1H-indazol-1-yl}pyrimidin-2-amine with 4-[6-bromo-3-(morpholin-4-ylmethyl)-1H-indazol-1-yl]pyrimidin-2-amine and 2-methyl-but-3-yn-2-ol with 2-(1,3-thiazol-2-yl)but-3-yn-2-ol. The reaction was carried out at 60° C. for 1.5 hr. Title compound was obtained: 1H NMR (500 MHz, DMSO) δ 1.93 (3H, s), 2.45 (4H, br. s.), 3.55-3.57 (4H, m), 3.88 (2H, s), 6.98 (2H, br. s.), 7.05 (1H, d, J=5.52 Hz), 7.12 (1H, s), 7.35 (1H, dd, J=8.35, 1.26 Hz), 7.68 (1H, d, J=3.31 Hz), 7.78 (1H, d, J=3.31 Hz), 8.01 (1H, d, J=8.35 Hz), 8.27 (1H, d, J=5.52 Hz), 8.87 (1H, s); LC-MS: m/z=+462.1 (M+H)+.

Provenance & Evidence