Mimicking the nature has always been a coveted target for scientific communinities. A precise understanding has emerged as to how enzymes accomplish the chemical transformations. Enzymes catalyze inert C-H bond functionalization in a regio- and stereoselective manner using metal-active site. Inspired by the nature, we have developed catalytic methods to functionalize carbon–hydrogen (C–H) bonds which provides significant economic and environmental benefits over traditional synthetic methods. Applicability of our strategies towards synthesis of various complex molecules will be discussed.