“…7 Representative examples of biologically relevant natural products and new chemical entities (NCEs) derived from the 3-methyleneisoindolin-1-one core are AKS 186 (I), 8 fumaridine (II), 9 narceine imide (III), 10 fumaramidine (IV), 11 fumaramine (V), 12 (R)-PD 172939 (dopamine D4 antagonist) (VI), 13 lennoxamine (VII), 14 aristoyagonine (VIII), 15 allosteric agent (IX), 16 and (S)-pazinaclone (X) 17 (Figure 1). In addition to methyleneisoindoline-1-ones, derivatives of thiochromene-4-imines also show a myriad of potential biological activities, such as antiproliferative, 18 antiemetic, 19 antioxidant, 20 antibacterial, 21 and anti-HIV, 22 which intensify the importance of new suitable approaches for the synthesis of these derivatives. One of the most efficient and convenient methods for the synthesis of methyleneisoindoline-1-ones and thiochromene-4-imines analogues include the ligand-promoted transition metal-catalyzed carbon−carbon or carbon-heteroatom coupling reaction, followed by additive cyclization on the triple bond.…”