•We review different strategies for achieving greener derivatization procedures.•We emphasize less hazardous reagents and solvents and more efficient energy.•We consider alternative media to classical organic solvents.•We discuss alternative forms of energy for activating derivatization processes. Principle 8 of Green Chemistry recommends eliminating derivatization, yet it is difficult to fulfill in analytical chemistry, so we consider the design of environment-friendly derivatization procedures in this article. We provide an overview on the main strategies for achieving greener derivatization procedures, emphasizing the use of less hazardous reagents and solvents and more efficient forms of energy. We consider using alternative media, such as water, bio-derived solvents, natural deep eutectic solvents, supercritical fluids, ionic liquids and organic solvents instead of classical undesirable solvents. We highlight derivatization with natural compounds and enzymes. We also discuss use in derivatization of different forms of energy, such as microwaves, ultrasound, photochemical or electrochemical. We present numerous examples where the overall green profile of the analytical methodology can be enhanced by focusing on the derivatization steps.