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Preparation of Oxysterols by C-H Oxidation of Dibromocholestane with Ru(Bpga) Catalyst.

Yui FujiiMakoto YoritateKana MakinoKazunobu IgawaDaiki TakedaDaiki DoiuchiKatsuhiko TomookaTatsuya UchidaGo Hirai
Published in: Molecules (Basel, Switzerland) (2021)
Seven mono- and dihydroxycholesterols were prepared by direct C-H oxidation of the cholestane skeleton with a recently developed Ru(Bpga) catalyst (Ru(Bpga) = [RuCl (bpga) (PPh 3 )] Cl; bpga = 2-(bis(pyridin-2-ylmethyl)amino)- N -(2,6-dimethylphenyl)acetamide)). Due to the high selectivity of the Ru(Bpga) complex for tertiary C-H, the reaction afforded a mixture of 25-, 20-, 17-, and 14-oxygenated cholesterols that could be easily separated by high-performance liquid chromatography. These results suggest that late-stage C-H oxidation could be a viable strategy for preparing candidate metabolites of biologically important molecules.
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