Concise Synthesis of Tetrazole Macrocycle

Eman M M Abdelraheem, Michel P de Haan, Pravin Patil, Katarzyna Kurpiewska, Justyna Kalinowska-Tłuścik, Shabnam Shaabani, Alexander Dömling

OnderzoeksoutputAcademicpeer review

21 Citaten (Scopus)
254 Downloads (Pure)


A concise two step synthesis of tetrazole containing macrocycles from readily accessible starting materials is presented. The first step comprises a chemoselective amidation of amino acid derived isocyanocarboxylicacid esters with unprotected symmetrical diamines to afford diverse α-isocyano-ω-amines. In the second step, the α-isocyano-ω-amines undergo an Ugi tetrazole reaction to close the macrocycle. Advantageously, this strategy allows short access to 11-19-membered macrocycles in which substituents can be independently varied at three different positions.

Originele taal-2English
Pagina's (van-tot)5078-5081
Aantal pagina's4
TijdschriftOrganic letters
StatusPublished - 13-sep.-2017

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