Expanding Synthesizable Space of Disubstituted 1,2,4-Oxadiazoles

ACS Comb. Sci. 2016, 18 (10), 616-624

DOI: 10.1021/acscombsci.6b00103

Tolmachev A.; Bogolubsky A. V.; Pipko S. E.; Grishchenko A. V.; Ushakov D. V.; Zhemera A. V.; Viniychuk O. O.; Konovets A. I.; Zaporozhets O. A.; Mykhailiuk P. K.; Moroz Y. S.

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.

Expanding Synthesizable Space of Disubstituted 1,2,4-Oxadiazoles


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