Phosphonium-mediated cyclization of N-(2-aminophenyl)thioureas: efficient synthesis of 2-aminobenzimidazoles |
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Authors: | Zhao-Kui Wan Erena Farah OusmanNikolaos Papaioannou Eddine Saiah |
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Institution: | Pfizer Worldwide Research and Development, Pfizer Inc., 200 Cambridge Park Drive, Cambridge, MA 02140, USA |
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Abstract: | BOP efficiently promoted the phosphonium-mediated cyclization of thioureas, leading to a convenient synthesis of 2-aminobenzimidazoles. Compared to conventional methods, the reactions were complete at room temperature with times ranging from a few minutes to 1 h in near quantitative yields. This method is also applicable to the synthesis of more challenging structures such as 2-akylaminobenzimidazoles and 2-(N-acyl)-aminobenzimidazoles. The methodology described herein represents a mild and efficient route to a variety of 2-aminobenzimidazoles. |
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Keywords: | Phosphonium-mediated cyclization Thioureas 2-Aminobenzimidazoles |
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