(2R)-1-aminopropan-2-ol → 4-({5-[(1R)-2-amino-1-methylethoxy]quinazolin-4-yl}amino)-2-chlorophenol

Participants

Reaction Steps

(R)-1-amino-2-propanol was reacted with 2-chloro-4-[(5-fluoroquinazolin-4-yl)amino]phenol (prepared as described in Example 4-4, preparation of starting materials) using an analogous process to that described Example 1 for the preparation of N-[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]-5-[2-(methylamino)ethoxy]quinazolin-4-amine) to give 4-({5-[(1R)-2-amino-1-methylethoxy]quinazolin-4-yl}amino)-2-chlorophenol in 64% yield; NMR spectrum (DMSO-d6) 1.39 (d, 3H), 2.88-3.03 (m, 2H), 3.72-3.85 (m, 1H), 6.95 (d, 1H), 7.15 (d, 1H), 7.29 (d, 1H), 7.45-7.52 (m, 1H), 7.69, (t, 1H), 8.05 (s, 1H), 8.45 (s, 1H) Mass spectrum MH+ 345.

Provenance & Evidence