Hydrochloric Acid → HCID 86634502, compound

Participants

Reaction Steps

To a cooled solution (0-5° C.) of (2S,4R)-tert-butyl 2-((2S,3S)-1-(cyclopropylamino)-2-hydroxy-1-oxohexan-3-ylcarbamoyl)-4-(7-methoxy-2-(1H-pyrazol-1-yl)quinolin-4-yloxy)pyrrolidine-1-carboxylate (3.0 g; 4.82 mmol) in methanol (10 mL) was added 17% methanolic hydrochloric acid (20 mL) dropwise. The reaction mixture was stirred at room temperature for 2 hours under nitrogen atmosphere. Completion of the reaction was monitored by TLC. Methyl t-butylether (50 mL) was added to the mixture and stirred for 10 minutes. The obtained solid was filtered and dried to yield 2.45 g (98%) of (2S,4R)-2-((2S,3S)-1-(cyclopropylamino)-2-hydroxy-1-oxohexan-3-ylcarbamoyl)-4-(7-methoxy-2-(1H-pyrazol-1-yl)quinolin-4-yloxy)pyrrolidinium chloride (HPLC purity: 97.74% by area; HPLC retention time: 13.30 minutes), which was used without further purification in the next step.

Provenance & Evidence