C-N bond formation is a particularly important step in the generation of many
biologically relevant heterocyclic molecules. Several methods have been reported for this
purpose over the past few decades. Well-known named reactions like Ullmann-Goldberg
coupling, Buchwald-Hartwig coupling and Chan-Lam coupling are associated with the C-N
bond formation reactions. Several reviews covering this topic have already been published.
However, no comprehensive review covering the synthesis of drugs/ lead compounds using
the C-N bond formation reactions was reported. In this review, we cover many modern
methods of the C-N bond formation reactions, with special emphasis on metal-free and
green chemistry methods. We also report specific strategies adopted for the synthesis of
drugs, which involve the C-N bond formation reactions. Examples include anti-cancer,
antidepressant, anti-inflammatory, anti-atherosclerotic, anti-histaminic, antibiotics, antibacterial, anti-rheumatic,
antiepileptic and anti-diabetic agents. Many recently developed lead compounds generated using the C-N bond
formation reactions are also covered in this review. Examples include MAP kinase inhibitors, TRKs inhibitors,
Polo-like Kinase inhibitors and MPS1 inhibitors.
