Several methods are available for the preparation of palladacycles. A simple and direct method is C–H activation. The cyclopalladation of aromatic derivatives is usually considered to go through an electrophilic aromatic substitution pathway. The oxidative addition of aryl halides is another useful method. However, the accessibility of the aryl halides starting material is a major drawback.
Other types of reactions such as transmetalation and nucleopalladation also turned out to be effective methods in the synthesis of palladacycles.