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Efficient approach for the diversity-oriented synthesis of macro-heterocycles on solid-support

✍ Scribed by Marc Giulianotti; Adel Nefzi

Publisher: Elsevier Science
Year: 2003
Tongue: French
Weight: 176 KB
Volume: 44
Category: Article
ISSN: 0040-4039
DOI: 10.1016/s0040-4039(03)01219-x

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✦ Synopsis

The generation of macro-heterocycles starting from resin bound orthogonally protected lysine and using nucleophilic aromatic substitution is described. The method of cyclization required the coupling of o-fluoro-p-nitro benzoic acid followed by intramolecular displacement of the fluoro group. The described method allows a versatile synthetic route to the synthesis of libraries of macro-heterocycles in an attempt to establish lead drug candidates. The desired cyclic products were obtained in good yields and purities.

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