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Updated: Oct 20, 2025

Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay
Published on: February 9, 2021
Pd-catalysed general access to 7-membered N/O-heterocyclic compounds as potential agents against inflammation
B Thirupataiah1,2, Gangireddy Sujeevan Reddy1,2, Guntipally Mounika1
1Dr. Reddy's Institute of Life Sciences, University of Hyderabad Campus, Gachibowli, Hyderabad 500 046, India. manojitpal@rediffmail.com.
Abstract:
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.
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Due to the absence of continuous...
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