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Two-Steps Hantzsch Based Macrocyclization Approach for the Synthesis of Thiazole Containing Cyclopeptides.

ABSTRACT: 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.

SUBMITTER: Nefzi A

PROVIDER: S-EPMC2989683 | biostudies-literature | 2010 Nov

REPOSITORIES: biostudies-literature

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Two-Steps Hantzsch Based Macrocyclization Approach for the Synthesis of Thiazole Containing Cyclopeptides.

Nefzi Adel A Arutyunyan Sergey S Fenwick Jason E JE

The Journal of organic chemistry 20101101 22

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. ...[more]

PMID: 21113437

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