| Literature DB >> 27548754 |
Andrey Tolmachev1,2, Andrey V Bogolubsky1, Sergey E Pipko2,3, Alexander V Grishchenko1, Dmytro V Ushakov1, Anton V Zhemera1, Oleksandr O Viniychuk3, Anzhelika I Konovets1,4, Olga A Zaporozhets5, Pavel K Mykhailiuk1,5, Yurii S Moroz2.
Abstract
One-pot synthesis of 3,5-disubstituted 1,2,4-oxadiazoles from carboxylic acids and nitriles was optimized to parallel chemistry. The method was validated on a 141 member library; the desired products were recovered with a high success rate and in moderate yields. Practical application of the approach was demonstrated in the synthesis of bioactive compound pifexole and agonists of free fatty acid receptor 1. A library of 4 948 100 synthesizable drug-like 3,5-disubstituted 1,2,4-oxadiazoles was enumerated based on the method and available validated reagents.Entities:
Keywords: 1,2,4-oxadiazoles; carboxylic acids; nitriles; one-pot parallel synthesis; readily accessible (REAL) arrays
Mesh：
Substances：
Year: 2016 PMID： 27548754 DOI： 10.1021/acscombsci.6b00103
Source DB: PubMed Journal: ACS Comb Sci ISSN： 2156-8944 Impact factor: 3.784