Metallaphotoredox aryl and alkyl radiomethylation for PET ligand discovery

The Deuterated “Magic Methyl” Group: A Guide to Site‐Selective Trideuteromethyl Incorporation and Labeling by Using CD3Reagents

“…MacMillan and co‐workers developed a method for methylation of aryl bromides and alkyl bromides under metallaphotoredox conditions in 2018 [88] . They developed their method further in later work to also facilitate radiomethylation of alkyl‐ and aryl bromides [89] . The main focus of the article is on late‐stage functionalization of pharmaceutical derivatives with CT 3 and 11 CH 3 units, but also one example was shown for CD 3 installation (Scheme 22b).…”

“… [88] They developed their method further in later work to also facilitate radiomethylation of alkyl‐ and aryl bromides. [89] The main focus of the article is on late‐stage functionalization of pharmaceutical derivatives with CT 3 and 11 CH 3 units, but also one example was shown for CD 3 installation (Scheme 22 b). For the original metallaphotoredox methylation protocol, a clear mechanism was proposed, but for the trideuteromethylation under slightly adapted conditions, the authors did not provide the particular mechanism.…”

Photo‐Induced Ruthenium‐Catalyzed C−H Benzylations and Allylations at Room Temperature

“…[8d] Visible-light metallaphotoredox catalysis constitutes a sustainable approach to allow for transformations under mild conditions. [9] Major contributions in this area were thus made by among others Akita, [10] MacMillan, [11] Molander, [12] Glorius, [13] König [14] and Doyle, [15] alkylations [16] as well as ortho-selective CÀ H arylations, [17] through exogenous photocatalyst-free ruthenium catalysis. Within our program on photo-induced CÀ H activation, [18] we have now developed unprecedented photo-induced CÀ H benzylations and allylations at ambient temperature (Figure 1c).…”

Highlight selection of radiochemistry and radiopharmacy developments by editorial board

“…The authors (Pipal et al, 2020) initially optimized the radiolabeling conditions using a [CT 3 ]methyl-1-naphthalene-sulfonate, a stable and non-volatile synthon for CT 3methylations. They were able to demonstrate high radiolabeling yields in a variety of substrates, including both aromatic and aliphatic C-C coupling reactions.…”