Relay tricyclic Pd(ii)/Ag(i) catalysis: Design of a four-component reaction driven by nitrene-transfer on isocyanide yields inhibitors of EGFR

ISSN
13597345
Date Issued
2018-01-01
Author(s)
Sawant, Devesh M.
Sharma, Shivani
Pathare, Ramdas S.
Joshi, Gaurav
Kalra, Sourav
Sukanya, Sukanya
Maurya, Antim K.
Metre, Ramesh K.
Agnihotri, Vijai K.
Khan, Shahnawaz
Kumar, Raj
Pardasani, R. T.
DOI
10.1039/c8cc05845h
Abstract
Synthesis of pyrazolo[1,5-c]quinazolines from four easily available precursors is presented through a one-pot tricyclic Pd(ii)/Ag(i) relay catalysis. The bimetallic relay cascade forges five new chemical bonds by concatenating six discrete chemical steps. The relay catalysis enables four-component assembly of pyrazolo[1,5-c]quinazolines that selectively inhibit EGFR, exhibit apoptosis through the ROS-induced mitochondrial-mediated pathway, and arrest the cell cycle at the G1 phase.