1.
Angew Chem Int Ed Engl
; 56(18): 5101-5105, 2017 04 24.
Artigo
em Inglês
| MEDLINE
| ID: mdl-28370927
RESUMO
A novel and catalyst-free multicomponent reaction with cyclic tertiary amines, electron-deficient aryl halides or heteroaromatic halides, and Na2 S enabled by facile C-N bond cleavage of the cyclic tertiary amines was developed. This direct and operationally simple method can be applied with a wide range of functional groups and provides an efficient and rapid approach to potentially drug-like products containing amine, azaarene, thioether, or phenol ether functionalities in good to excellent yields. The utility of this method was demonstrated by the rapid synthesis of the analgesic ruzadolane.