Pd/C-mediated Synthesis of 3-methyleneisoindolin-1-ones: Biological and Theoretical Study of their PDE4 Inhibition
Suryadevara Vijayavardhini, Dandela Rambabu, Vegendla Anuradha, Ravikumar Kapavarapu, Mandava Venkata Basaveswara Rao and Manojit Pal
Affiliation: Dr. Reddy’s Institute of Life Sciences, University of Hyderabad Campus, Hyderabad-500 046, India.
Keywords: Alkynes, Pd/C, coupling, 3-methyleneisoindolin-1-ones.
Pd/C-Cu mediated alternative and one-pot method has been developed for the synthesis of (Z)-3-
methyleneisoindolin-1-ones as potential inhibitors of PDE4. The methodology involved coupling-cyclization of obromobenzamides
with a range of terminal alkynes in a single pot to afford the target compounds in acceptable yields.
Some of these compounds showed encouraging inhibition of PDE4 when tested in vitro that was supported by in silico
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