Recently, graphene and graphene-based nanomaterials have emerged as advanced carbon functional materials with specialized unique electronic, optical, mechanical, and chemical properties. These properties have made graphene an exceptional material for a wide range of promising applications in biological and non-biological fields. The present review illustrates the structural modifications of pristine graphene resulting in a wide variety of derivatives. The significance of substitutional doping with alkali-metals, alkaline earth metals, and III–VII group elements apart from the transition metals of the periodic table is discussed. The paper reviews various chemical and physical preparation routes of graphene, its derivatives and graphene-based nanocomposites at room and elevated temperatures in various solvents. The difficulty in dispersing it in water and organic solvents make it essential to functionalize graphene and its derivatives. Recent trends and advances are discussed at length. Controlled reduction reactions in the presence of various dopants leading to nanocomposites along with suitable surfactants essential to enhance its potential applications in the semiconductor industry and biological fields are discussed in detail.