Skip to content

Bromination of ketones

Klementine Burrell-Sander edited this page Sep 12, 2024 · 5 revisions

The protocol used is linked at the start of each attempt listed.

KBS38 (2-bromo-1-(6-bromopyridin-2-yl)ethan-1-one)

KBS38-1 - NBS method, 90% conversion

KBS38-2 - HBr method, 67% conversion

KBS38-3 - 89% NBS method

KBS38-3 - 95% NBS method

KBS39 (2-bromo-1-(quinolin-2-yl)ethan-1-one) - all NBS

KBS39-1 - 32%

KBS39-2 - 35%

KBS40 (2-bromo-1-(5-bromopyridin-2-yl)ethan-1-one) - all NBS

KBS40-1 - 89%

KBS40-2 - 94%

KBS40-3 - 87%

KBS41 (2-bromo-1-(5-phenylpyridin-2-yl)ethan-1-one) - all NBS

KBS41-1 - 72%

KBS41-2 - 77%

KBS42 (2-bromo-1-(4-chloropyridin-2-yl)ethan-1-one) - all NBS

KBS42-1 - 71%

KBS42-2 - product not recovered

KBS42-3 - tbd

KBS42-4 - 77%

Notes

Started off with NBS/tosic acid. This is not the radical Wohl-Ziegler type reaction. Previous efforts to brominate ketones required the use of HBr in acetic acid/Br2 - this will be the second route explored.

Another alternative is CuBr2 in ethyl acetate (ref 1, ref 2.) but this seems to primarily work on phenyl compounds.

NBS/tosic acid method is established to work on phenyl compounds. It is possible that the nitrogen complicates the reaction in the case of pyridinyl ketones. E.g. see ref 1 where CuBr2 is used for phenyl compounds but HBr is used for pyridinyl rings. Also ref 3.

Pyridinium tribromide is sometimes used an alternative source of Br (in place of Br2) - see ref 4.

Clone this wiki locally