Publications by authors named "Rajeesh Pakkath"
Article Synopsis
- A new catalytic method was developed for synthesizing 7-(hetero) aryl-1H-pyrrolo[2,3-c]pyridine compounds using microwave-assisted Suzuki-Miyaura cross-coupling, achieving excellent yields.
- The method effectively utilizes various boronic acids and potassium organotrifluoroborates, highlighting the importance of stable monoligated catalytic species for successful reactions.
- A highly efficient precatalytic system (XPhos-PdG2) was employed, which facilitates rapid reaction rates with low catalyst amounts, demonstrating the method's versatility with 7-chloro, 6-azaindole systems featuring free N-H groups.
In this paper we report the SAR studies of a series of N-(4-(4-chloro-1H-imidazol-1-yl)-3-methoxyphenyl)amide and N-(4-(4-chloro-1H-imidazol-1-yl)-3-methoxyphenyl)sulfonamide derivatives 6(a-o) and 7(a-o), were synthesized in good yields and characterized by (1)H NMR, (13)C NMR and mass spectral analyses. The preparation of the key intermediate highlights an optimized palladium catalyzed (Pd₂(dba)₃/RuPhos) Buchwald cross-coupling of intermediate 2 and 3. The newly synthesized compounds were evaluated for their in vitro antibacterial activity against Staphylococcus aureus, (Gram-positive), Escherichia coli and Klebsiella pneumoniae (Gram-negative), antifungal activity against Candida albicans, Aspergillus flavus and Rhizopus sp.
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