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.
Fast Heck−Cassar−Sonogashira (HCS) Reactions in Green Solvents / Ferrazzano L; Martelli G; Fantoni T; Daka A; Corbisiero D; Viola A; Ricci A; Cabri W; Tolomelli A. - In: ORGANIC LETTERS. - ISSN 1523-7060. - ELETTRONICO. - 22:10(2020), pp. 3969-3973. [10.1021/acs.orglett.0c01269]
Fast Heck−Cassar−Sonogashira (HCS) Reactions in Green Solvents
Ferrazzano L;Martelli G;Fantoni T;Corbisiero D;Cabri W;Tolomelli A
2020
Abstract
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.| File | Dimensione | Formato | |
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