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Open AccessFeature PaperArticle

The First Catalytic Direct C–H Arylation on C2 and C3 of Thiophene Ring Applied to Thieno-Pyridines, -Pyrimidines and -Pyrazines

Institut de Chimie Organique et Analytique (ICOA), Université d’Orléans UMR-CNRS 7311, BP 6759, rue de Chartres, 45067 Orléans CEDEX 2, France
Departmento/Centro de Química, Escola de Ciências, Universidade do Minho, Campus de Gualtar, 4710-057 Braga, Portugal
Author to whom correspondence should be addressed.
Catalysts 2018, 8(4), 137;
Received: 13 March 2018 / Revised: 27 March 2018 / Accepted: 28 March 2018 / Published: 30 March 2018
(This article belongs to the Special Issue Catalyzed Mizoroki–Heck Reaction or C–H activation)
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A practical one-pot procedure for the preparation of diverse thieno[3,2-d]pyrimidines is reported here for the first time. This two-step process via C–H activation in position C-2 of thiophene led to the development of an improved methodology for the synthesis of numerous compounds. This new methodology is an efficient alternative to the conventional methods currently applied. The C–H activation of the thiophene C-3 position was also achieved and can be selective. The optimized conditions can also be applied to thienopyridines and thienopyrazines. View Full-Text
Keywords: C–H activation; regioselectivity; thienopyridines; thienopyrimidines; thienopyrazines C–H activation; regioselectivity; thienopyridines; thienopyrimidines; thienopyrazines

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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).

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Campos, J.F.; Queiroz, M.-J.R.P.; Berteina-Raboin, S. The First Catalytic Direct C–H Arylation on C2 and C3 of Thiophene Ring Applied to Thieno-Pyridines, -Pyrimidines and -Pyrazines. Catalysts 2018, 8, 137.

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