Photocatalytic three-component asymmetric sulfonylation via direct C(sp3)-H functionalization

Abstract The direct and selective C(sp 3 )-H functionalization of cycloalkanes alkanes is a highly useful process in organic synthesis owing to the low-cost starting materials, high step atom economy. Its application asymmetric catalysis, however, has been scarcely explored. Herein, we disclose our effort toward this goal by incorporation dual photocatalysis chiral nickel catalyst commercially available organophotocatalyst with radical relay strategy through sulfur dioxide insertion. Such design leads development three-component sulfonylation involving cycloalkanes, alkanes, toluene derivatives or ethers. photochemical reaction precursor, SO 2 surrogate common ?,?-unsaturated carbonyl compound proceeds smoothly under mild conditions, delivering wide range biologically interesting ?-C sulfones regio- enantioselectivity (>50 examples, up >50:1 rr 95% ee). This method applicable late-stage bioactive molecules, provides an appealing access enantioenriched compounds from abundant hydrocarbon compounds.