학술논문
Introduction of Trifluoroethylamine as Amide Isostere by C-H Functionalization of Heteroarenes.
Document Type
Abstract
Source
Subject
*HETEROARENES
*AMIDES
*FUNCTIONAL groups
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Language
ISSN
1523-7060
Abstract
A direct and efficient introduction of a trifluoroethylamine motif into various heteroaromatic structures, using a readily available xanthate S-[1-(N-acetylamino)-2,2,2-trifluoroethyl]-O-ethyl dithiocarbonate (5), is reported. Medicinally relevant trifluoroethylaminated heteroarenes containing a wide range of functional groups were successfully synthesized under mild conditions. This amide isostere could be introduced into both electron-rich and -poor heteroarenes to give the desired products in one step. The beneficial effect of camphorsulfonic acid (CSA) was also demonstrated with electron-deficient heteroarenes. [ABSTRACT FROM AUTHOR]