RT Journal Article
T1 Pd(II)-catalyzed conjugate addition of boronic acids to ketoglutaconic esters toward the synthesis of functionalized pridazin-3(2H)-ones with neuroprotective activity
A1 Roscales García, Silvia
A1 Ortega, Andrea
A1 Martín-Aragón Álvarez, Sagrario
A1 Bermejo Bescos, María De La Paloma
A1 García Csaky, Aurelio
AB The development of the regioselective conjugate addition of boronic acids to ketoglutaconic esters under transition metal catalysis is reported. Among the different catalysts tested for this transformation, the dicationic PdII catalysts generated with Pd(OCOCF3)2, dppben, and HBF4 performed best in terms of yields, regioselectivities and avoidance of Heck-type by-products. The resulting 4-aryl-2-oxopentadienoates were transformed into pyridazin-3(2H)-ones, potentially useful for the therapy of neurodegenerative diseases. These compounds simultaneously exhibited β-secretase activity, inhibition of β-amyloid (βA) aggregation, and disaggregation of pre-formed βA fibrils, and also had a good scavenging profile for intracellular reactive oxygen species (ROS).
YR 2012
FD 2012
LK https://hdl.handle.net/20.500.14352/115356
UL https://hdl.handle.net/20.500.14352/115356
LA eng
DS Docta Complutense
RD 15 abr 2025