Solid-phase synthesis of 5'-deoxy-5'-amino-clitocine analogues |
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Authors: | Varaprasad Chamakura V N S Habib Qazi An Haoyun Hong Zhi |
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Institution: | Department of Medicinal Chemistry, Valeant Pharmaceuticals International, Inc., 3300 Hyland Avenue, Costa Mesa, CA 92626, USA. vchamakura@valeant.com |
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Abstract: | Several 6-substituted-amino-5'-deoxy-5'-amino-clitocine analogues were synthesized in a parallel fashion in solid phase. The desired scaffold was generated by coupling 2,3-O-bis-(t-butyldimethylsilyl)-5-N-(monomethoxytrityl-polystyrene-resin)-1,5-diamino-5-deoxy-beta-D-ribofuranose and 4, 6-dichloro-5-nitropyrimidine. The scaffold was then reacted with a variety of amines to generate a small library of 14 analogues of 5'-deoxy-5'-amino-clitocine following a protocol developed earlier. |
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