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

25 July 2022, Version 1
This content is a preprint and has not undergone peer review at the time of posting.

Abstract

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%.

Keywords

fluorine
fluoromethyl
heteroaromatic
difluoroacetone
cyclization
amino pyridine

Supplementary materials

Title
Description
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Title
Synthesis of mono-fluoromethyl 6,5-heteroaromatic bicycles using 1,3-difluoroacetone as a cyclising reagent
Description
Experimental procedures, analytical conditions, and characterization data
Actions

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