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Abstract
We have repurposed the Huisgen rearrangement towards a multicomponent synthesis of 2-amino-1,3,4-thiadiazoles and 2-amino-1,3,4-oxadiazoles. The starting materials – 5-sustituded-1H-tetrazoles, TCDI or CDI, and amines – are readily accessible and allow for modular construction of heterocyclic scaffolds. To demonstrate the enabling aspect of this transformation towards late-stage modification of medicinally relevant molecules, we have prepared a thiadiazole-containing crisaborole derivative.
Supplementary materials
Title
Multicomponent assembly of heterocycles
Description
We have repurposed the Huisgen rearrangement towards a multicomponent synthesis of 2-amino-1,3,4-thiadiazoles and 2-amino-1,3,4-oxadiazoles. The starting materials – 5-sustituded-1H-tetrazoles, TCDI or CDI, and amines – are readily accessible and allow for modular construction of heterocyclic scaffolds. To demonstrate the enabling aspect of this transformation towards late-stage modification of medicinally relevant molecules, we have prepared a thiadiazole-containing crisaborole derivative.
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