An Efficient Approach to Aromatic Aminomethylation Using Dichloromethane as Methylene Source

Frontiers in Chemistry

Carmine Ostacolo¹  Isabel M. Gomez Monterrey¹  Alessia Bertamino²  Vincenzo Vestuto²  Giacomo Pepe²  Veronica Di Sarno²  Fabrizio Merciai²  Tania Ciaglia²  Simona Musella³  Pietro Campiglia³ 

[1] Department of Pharmacy, University of Naples “Federico II”, Naples, Italy;Department of Pharmacy, University of Salerno, Fisciano, Italy;Fondazione EBRIS, Salerno, Italy;

关键词: aminomethylation;    ultrasound assisted;    dichloromethane;    indole N-1 selectivity;    aza-heterocyclic compounds;   

DOI  :  10.3389/fchem.2019.00568

来源: DOAJ

【 摘 要 】

Ultrasound-promoted N-aminomethylation of indoles can be achieved in basic medium using sodium hydride and dichloromethane (DCM) as C1 donor source. This innovative amino methylation protocol results in good to excellent yields of multifunctional indole derivatives. The procedure is also applicable to other aza-heterocyclic compounds and, interestingly, affords direct access to aminomethyl-substituted aryl alcohols.

【 授权许可】

Unknown