Monastrol (M) is an important target molecule for organic chemists in virtue of its remarkable biological properties, e.g. antitumoral activity [1] and inhibition of the motility of the mitotic motor protein kinesin Eg5, thus serving as a particularly useful tool for study of mitotic mechanisms [2]. The most useful and smart method actually applied for M synthesis is the Biginelli multicomponent reaction (MCR), discovered in 1891 by Pietro Biginelli [3]. MCRs have the advantage of performing the reaction in a one-pot version, thus avoiding waste from multistep purifications and residue generation. Moreover, MCR adducts include in their structures almost all atoms (atom economy), the common by-product being water. Current communication will present some recent advances described in the literature, regarding the convenient synthesis of M, based on the environmentally benign methods in sustainable conditions [4-6]. Schematic representation of Biginelli reaction applied for the preparation of (+/-)-Monastrol in eco-friendly conditions