Two-Steps Hantzsch Based Macrocyclization Approach for the Synthesis of Thiazole Containing Cyclopeptides.
Article
Nefzi, Adel, Arutyunyan, Sergey, Fenwick, Jason E. (2010). Two-Steps Hantzsch Based Macrocyclization Approach for the Synthesis of Thiazole Containing Cyclopeptides.
. JOURNAL OF ORGANIC CHEMISTRY, 75(22), 7939-7941. 10.1021/jo1016822
Nefzi, Adel, Arutyunyan, Sergey, Fenwick, Jason E. (2010). Two-Steps Hantzsch Based Macrocyclization Approach for the Synthesis of Thiazole Containing Cyclopeptides.
. JOURNAL OF ORGANIC CHEMISTRY, 75(22), 7939-7941. 10.1021/jo1016822
Macrocyclization via an efficient high-yielding solid-phase intramolecular thioalkylation reaction is described. The reaction of S-nucleophiles with newly generated N-terminal 4-chloromethyl thiazoles led to the desired macrocyclization products 5 in high purities and good overall yields.