Synthesis of mono-fluoromethyl 6,5-heteroaromatic bicycles using 1,3-difluoroacetone as a cyclising reagent [post]

Longbin Liu, Brett Cosgrove, Cole Clissold, Karine Malagu, Mark Chambers, Celia Dominguez
2022 unpublished
The development of facile, wide scope synthetic methodologies providing access to fluorinated motifs is important in medic-inal chemistry; for our purposes, we are interested in developing fluorine-tagged compounds to investigate their utility in Huntington's disease. Here, we describe a novel, operationally simple and mild procedure for the synthesis of mono-fluoromethyl 6,5-heteroaromatic bicycles using 1,3-difluoroacetone (DFA). The scope of the reaction was investigated, and 27 examples synthesized with yields up to 96%.
doi:10.26434/chemrxiv-2022-c03kc-v3 fatcat:yti35zboqnduppsyqosjkolvw4