Methanesulfonamide → HCID 46947711, compound

Participants

Reaction Steps

A mixture of 2-(4-(7-(bis((2-(trimethylsilyl)ethoxy)methyl)amino)-6-bromo-3-(quinolin-3-yl)pyrazolo[1,5-a]pyrimidin-5-yl)cyclohexyl)acetic acid (60 mg, 0.081 mmol), methanesulfonamide (12 mg, 0.122 mmol), 4-dimethylaminopyridine (20 mg, 0.163 mmol) and 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide hydrochloride (32 mg, 0.163 mmol) in dichloromethane (2.0 ml) was stirred at room temperature for 16 h. The reaction mixture was concentrated in vacuo. The crude mixture was dissolved in methanol (2 ml) and treated with 1N hydrochloride solution (2 ml) at 65° C. for 2 h. The reaction solution was concentrated and purified by prep-LC to afford the title compound (two isomers, cis and trans). Isomer 1: LC/MS RT=3.63 min. Mass calculated for, M+H 557.09, observed 557.09. Isomer 2: LC/MS RT=3.88 min. Mass calculated for, M+H 557.09, observed 557.09.

Provenance & Evidence