Acetic Acid → (3R,5S)-1-Acetyl-5-[({4-[3-chloro-4-fluoroanilino]-7-methoxyquinazolin-5-yl}oxy)methyl]pyrrolidin-3-ol

Participants

Reaction Steps

The procedure described in Example 25 was repeated using (3R,5S)-5-[({4-[3-chloro-4-fluoroanilino]-7-methoxyquinazolin-5-yl}oxy)methyl]pyrrolidin-3-ol (209 mg) with acetic acid (32 μl) to give the title compound as a white solid in 92% yield; NMR spectrum (DMSO-d6) 9.98 (s, 1H), 8.47 (s, 1H), 8.16-8.14 (m, 1H), 7.73-7.70 (m, 1H) 6.84 (s, 1H), 5.10 (m, 1H), 4.67-4.63 (m, 1H), 4.47-4.38 (m, 2H), 4.26-4.21 (m, 1H), 3.94 (s, 3H), 3.59 (dd, 1H), 3.41 (dd, 1H), 2.11-2.05 (m, 2H), 2.00 (s, 3H); Mass spectrum MH+ 461.

Provenance & Evidence