4-(Chlorosulfonyl)benzoic acid → HCID 86679575, compound

Participants

Reaction Steps

(S)-4-(2-(2-aminoacetoxy)-2-(3-(cyclopropylmethoxy)-4-(difluoromethoxy)-phenyl)ethyl)-3,5-dichloropyridine 1-oxide (prepared in an analogous manner as described in Scheme 1, Step 1-2) (100 mg, 0.210 mmol) was dissolved in py (2.5 ml). 4-(chlorosulfonyl)benzoic acid (60.1 mg, 0.272 mmol) was added, and the reaction was stirred at RT for 4 hours. The reaction mixture was diluted with HCl 1N and extracted with EtOAc. The organic phase was washed with HCl 1N and brine, dried over Na2SO4 and concentrated under vacuum to give (S)-4-(2-(2-(4-carboxyphenylsulfonamido)acetoxy)-2-(3-(cyclopropylmethoxy)-4-(difluoromethoxy)phenyl)ethyl)-3,5-dichloropyridine 1-oxide (120 mg, 87% yield).

Provenance & Evidence