TFA-sensitive arylsulfonylthiourea-assisted synthesis of N,N'-substituted guanidines |
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| Authors: | Li Jizhen Zhang Guangtao Zhang Zhongsheng Fan Erkang |
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| Affiliation: | Biomolecular Structure Center, Department of Biochemistry, University of Washington, Seattle, Washington 98195, USA. |
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| Abstract: | An efficient synthesis of N,N'-substituted guanidine derivatives was developed via an aromatic sulfonyl-activated thiourea intermediate. The use of certain aromatic sulfonamides, such as PbfNH(2), as the key reagent to incorporate a TFA-labile guanidine protection group greatly facilitates solid-phase synthesis of N,N'-substituted guanidine compounds. |
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