posted on 2020-04-28, 11:39authored byL. Ferrazzano, G. Martelli, T. Fantoni, A. Daka, D. Corbisiero, A. Viola, A. Ricci, W. Cabri, A. Tolomelli
The replacement of
toxic solvents with greener alternatives in
Heck–Cassar–Sonogashira (HCS) cross-couplings was investigated.
The fine-tuning of the HCS protocol allowed to achieve complete conversions
and high speed under mild conditions. N-Hydroxyethylpyrrolidone
(HEP) gave the best results. Moreover, the methodology was successfully
applied to the synthesis of an intermediate of the anticancer drug
Erlotinib, demonstrating the versatility of the new green protocol.