1,2-Dichloroethane → (S)-4-(2-(2-(2-(3-(N-(tert-butoxycarbonyl)-methylsulfonamido)-4-(cyclopropylmethoxy)phenyl)acetoxy)acetoxy)-2-(3-(cyclopropylmethoxy)-4-(difluoromethoxy)phenyl)ethyl)-3,5-dichloropyridine 1-oxide

Participants

Reaction Steps

To a solution of 2-(3-(N-(tert-butoxycarbonyl)methylsulfonamido)-4-(cyclopropylmethoxy)phenyl)acetic acid (0.200 g, 0.501 mmol) in DCM (5 ml), (S)-3,5-dichloro-4-(2-(3-(cyclopropylmethoxy)-4-(difluoromethoxy)phenyl)-2-(2-hydroxyacetoxy)ethyl)pyridine 1-oxide (0.239 g, 0.501 mmol), EDC (0.288 g, 1.502 mmol), and DMAP (0.0306 g, 0.250 mmol) were added, and the mixture was reacted for 5 hours. A 1N solution of HCl was added, and the desired compound was extracted with DCM (3×) recovering the crude desired product (0.450 g, yield considered to be quantitative, MS/ESI+ 859.3 [MH]+) that was used in the following step without further purification.

Provenance & Evidence