Ethanol → (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

Participants

Reaction Steps

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).

Provenance & Evidence