Enantioselective
Synthesis of Pyrazolo[3,4‑b]pyridone Derivatives
with Antifungal Activities against Phytophthora capsici and Colletotrichum fructicola
posted on 2022-12-23, 20:45authored byGuihua Nie, Jun Sun, Chengli Mou, Kun Tang, Yonggui Robin Chi, Tingting Li
A chiral NHC-catalyzed [3 + 3] cycloaddition
reaction
is developed
for the efficient synthesis of pyrazolo[3,4-b]pyridones
in generally excellent yields and optical purities. The R, S, and racemic forms of these molecules are systematically
studied via in vitro tests that detect antifungal
activity against Phytophthora capsici and Colletotrichum fructicola. Chiral compounds (R)-3i, (R)-3j, and (R)-3p are identified to have excellent inhibitory
effects against P. capsici and C. fructicola.