Access to distal meta-C-H functionalization of arylmethanesulfonic acid derivatives.

Herein, we report the meta-C-H olefination of arylmethanesulfonates aided by a potentially versatile aliphatic nitrile-directing group under microwave irradiation conditions with fair to very good yields and good to outstanding regioselectivities. Significantly, the protocol showed broad substrate scope including olefin-derived drugs and cyclic olefins. Remarkably, a dual meta-C-H bond was amenable to generating the bis-olefination products.

Functionalization of arylacetic acids via directing-group-assisted remote meta-C-H activation.

Herein, we report the first microwave-assisted remote-C-H functionalization aided by a simple nitrile directing template. Notably, the present protocol showed a broad substrate scope VIA enabling meta-C-H arylation, acetoxylation, and cyanation. Significantly, the microwave-accelerated meta-C-H functionalization was effective with short reaction times without compromising yields and site selectivity. In addition, ibuprofen drug diversification was accomplished by carrying out arylation, acetoxylation, and cyanation. Importantly, meta-dual-hetero functionalization has been presented.