Synthesis of aryldifluoromethyl aryl ethers via nickel-catalyzed suzuki cross-coupling between aryloxydifluoromethyl bromides and boronic acids
oleh: Heng Lu, Ruo-Xuan Xiao, Chang-Yun Shi, Zi-Lan Song, Hou-Wen Lin, Ao Zhang
| Format: | Article |
|---|---|
| Diterbitkan: | Nature Portfolio 2022-07-01 |
Deskripsi
Aryldifluoromethyl aryl ethers (ArCF2OAr’) are powerful structural motifs to improve druggability, however, their targeted synthesis remains challenging. Here, the authors report the efficient synthesis of ArCF2OAr’ motifs via nickel-catalyzed aryloxydifluoromethylation with arylboronic acids, and their application in the total synthesis of a difluoromethylated PD-1/PD-L1 immune checkpoint inhibitor with enhanced antitumor efficacy over the non-fluoro congener.