反应详情

A flask was charged with 0.5 mL of (S)-2-amino-3-(4-(2-amino-6-((R)-1-(4-chloro-2-(3-methyl-1H-pyrazol-1-yl)phenyl)-2,2,2-trifluoroethoxy)pyrimidin-4-yl)phenyl)propanoic acid free base (0.05 M, 0.025 mmol) in MeOH, and 0.28 mL ethanesulfonic acid in IPA (0.1N, 0.028 mmol, 1.1 equiv.). After the solvent was evaporated, 0.75 mL MeCN was added and stirred to give a suspension, followed by adding 0.2 mL EtOH and heated until the solid was completely dissolved. After stirring overnight, the crystal was filtered off, washed with heptane (0.6 mL), dried at 45° C. under vacuum to give (S)-2-amino-3-(4-(2-amino-6-((R)-1-(4-chloro-2-(3-methyl-1H-pyrazol-1-yl)phenyl)-2,2,2-trifluoroethoxy)pyrimidin-4-yl)phenyl)propanoic acid esylate (69% yield).

1. customAfter the solvent was evaporated
2. addition0.75 mL MeCN was added
3. customto give a suspension
4. temperatureheated until the solid
5. dissolutionwas completely dissolved
6. stirringAfter stirring overnight
7. filtrationthe crystal was filtered off
8. washwashed with heptane (0.6 mL)
9. customdried at 45° C. under vacuum