30063-80-0Relevant articles and documents
Expanding Synthesizable Space of Disubstituted 1,2,4-Oxadiazoles
Tolmachev, Andrey,Bogolubsky, Andrey V.,Pipko, Sergey E.,Grishchenko, Alexander V.,Ushakov, Dmytro V.,Zhemera, Anton V.,Viniychuk, Oleksandr O.,Konovets, Anzhelika I.,Zaporozhets, Olga A.,Mykhailiuk, Pavel K.,Moroz, Yurii S.
, p. 616 - 624 (2016)
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.
