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Issue 97, 2015
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A high-throughput synthesis of 1,2,4-oxadiazole and 1,2,4-triazole libraries in a continuous flow reactor

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Abstract

We report herein a high-throughput methodology for the synthesis of 1,2,4-oxadiazole and 1,2,4-triazole small-molecule libraries using an integrated synthesis and purification platform. The heterocyclization relies first on a low-temperature peptide coupling of a diverse set of carboxylic acids and hydroxyamidines, hydrazonamides, or pyridyl hydrazides followed by a high-temperature cyclization to yield the respective heterocycles in a continuous flow process. The fully integrated synthesis and purification platform enables the rapid generation of chemical libraries, decreasing the drug discovery cycle time.

Graphical abstract: A high-throughput synthesis of 1,2,4-oxadiazole and 1,2,4-triazole libraries in a continuous flow reactor

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Article information


Submitted
20 Aug 2015
Accepted
10 Sep 2015
First published
10 Sep 2015

RSC Adv., 2015,5, 79264-79269
Article type
Communication

A high-throughput synthesis of 1,2,4-oxadiazole and 1,2,4-triazole libraries in a continuous flow reactor

A. R. Bogdan and Y. Wang, RSC Adv., 2015, 5, 79264
DOI: 10.1039/C5RA18386C

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