Ru-Catalyzed C-H alkenylation on the arene ring of pirfenidone using pyridone as a directing group.
Chem Commun (Camb)
; 58(21): 3481-3484, 2022 Mar 10.
Article
em En
| MEDLINE
| ID: mdl-35191453
ABSTRACT
A method to functionalize the arene ring of pirfenidone has been demonstrated using pyridone as a directing group. Unlike the functionalization of the pyridone nucleus, the method demonstrated here is the alkenylation of the N-aryl ring of pirfenidone with internal alkynes using ruthenium catalyst. High functional group tolerance, simple reaction conditions and site-selective functionalization permit the synthesis of new analogues of drugs in a step-economical manner. The data of the control experiments suggest the possibilities of a base-assisted internal electrophilic substitution (BIES) pathway.
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MEDLINE
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En
Ano de publicação:
2022
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Article