1,2-Dichloroethane → HCID 89455778, compound

Participants

Reaction Steps

((S)-4-(2-(2-aminoacetoxy)-2-(3-(cyclopropylmethoxy)-4-(difluoromethoxy)-phenyl)ethyl)-3,5-dichloropyridine 1-oxide hydrochloride) (103 mg; 0.2 mmol) was dissolved in DMF (1.5 ml), then 3-(N-(tert-butoxycarbonyl)methylsulfonamido)-4-(cyclopropylmethoxy)benzoic acid (80 mg, 0.2 mmol), (for a reference procedure see Example 18, WO 2010/089107, which is incorporated herein by reference in its entirety), EDC (80 mg, 0.42 mmol), and DMAP (60 mg, 0.49 mmol) were added. The reaction was stirred at RT overnight, then was diluted with HCl 1M and extracted with EtOAc. The organic phase was washed with HCl 1M and with K2CO3 sat, dried over Na2SO4 and evaporated under vacuum to give 180 mg of the desired product (Yield: quantitative).

Provenance & Evidence