Regioselective N-Trideuteromethylation of Tautomeric Polyaza Heterocycles.
J Org Chem
; 89(11): 7780-7789, 2024 Jun 07.
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| MEDLINE
| ID: mdl-38752832
ABSTRACT
Methods for regioselective N-trideuteromethylation of tautomeric polyaza heterocycles are highly sought-after. Disclosed herein is an N-trideuterated methylation reaction of imidazoles and pyrazoles with high regioselectivity and deuterium purity using easily available CF3SO3CD3 as the -CD3 source. This method enables the easy synthesis of important deuterium-labeled azoles, including dimetridazole-d3, ipronidazole-d3, hydroxy dimetridazole-d3, and ronidazole-d3.
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2024
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