Pd-catalysed general access to 7-membered N/O-heterocyclic compounds as potential agents against inflammation

Autor: Jetta Sandeep Kumar, B. Thirupataiah, Jayesh Mudgal, Gangireddy Sujeevan Reddy, Guntipally Mounika, Kazi Amirul Hossain, Marina Rajadurai, Jessy Elizabeth Mathew, Gautham G. Shenoy, Kishore V. L. Parsa, Manojit Pal
Rok vydání: 2021
Předmět:
Zdroj: Chemical Communications. 57:10091-10094
ISSN: 1364-548X
1359-7345
Popis: A Pd-catalysed regioselective synthesis of 4,5-disubstituted 7-membered N/O-heterocycles was achieved via the 7-endo-dig cyclization followed by C–C bond formation of 2-(1-alkynyl)phenylacetamide. The ligand/additive free cascade reaction proceeded in the presence of PdCl2 in aqueous MeCN when the separate and individual use of methyl vinyl ketone and allyl bromide generally afforded an O- and N-heterocycle, respectively. The pharmacological assay was performed to identify the first example of a 1H-benzo[d]azepin-2(3H)-one based novel inhibitor of PDE4B.
Databáze: OpenAIRE