Hantzsch Based Macrocyclization Approach for the Synthesis of Thiazole Containing Cyclopeptides
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An innovative macrocyclization approach via high-yielding solid-phase intramolecular thioalkylation reaction is described.
The reaction of S
-nucleophiles with newly generated N-terminal 4-chloromethyl thiazoles leads to the desired cyclic products in high purities
and good yields.


![N-(cyclopropanesulfonyl)-5-cyclopropyl-2-[(cyclopropylmethyl)[(1R)-1-[5'-methyl-2'-(5-oxo-2,5-dihydro-1,2,4-oxadiazol-3-yl)-[1,1'-biphenyl]-4-yl]ethyl]amino]-1,3-thiazole-4-carboxamide,Moligand™,阿拉丁](https://img1.dxycdn.com/p/s14/2024/0619/785/8670042233826733081.jpg!wh200)






