Efficient synthesis of tetramethylsulfonylguanidines between a free sulfonamide group and HBTU |
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| Authors: | Sébastien Gluszok Jean-Pierre Hénichart |
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| Institution: | Institut de Chimie Pharmaceutique Albert Lespagnol, Université de Lille 2, EA 2692, IFR 114, 3, rue du Professeur Laguesse, B.P. 83, F-59006 Lille, France |
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| Abstract: | The reaction of a sulfonamide moiety with HBTU (O-(1H-benzotriazol-1-yl)-N,N,N′,N′-tetramethyluronium hexafluorophosphate) during amide coupling, leading to the formation of tetramethylsulfonylguanidines, is described. Optimised conditions showed that HBTU was as a convenient agent for the synthesis of tetramethylsulfonylguanidines, in basic conditions. A panel of diverse sulfonamides was used to demonstrate the scope of this procedure. |
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| Keywords: | HBTU Sulfonamide Tetramethylsulfonylguanidines |
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