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Indole-3-carboxaldehyde is a versatile compound with diverse applications in organic synthesis and medicinal chemistry. It serves as a crucial building block for the preparation of various indole derivatives, including complex molecules with significant biological activities. One notable application of indole-3-carboxaldehyde is its involvement in Schiff base condensation reactions, leading to the formation of multifunctional silica nano-vehicles and magnetic nanoparticles. These nanostructures hold promise in various fields, including drug delivery and catalysis. In organic synthesis, indole-3-carboxaldehyde is utilized as a starting material for the synthesis of several higher-order indoles, such as isoindolo[2,1-a]indoles, aplysinopsins, and 4-substituted-tetrahydrobenz[cd]indoles. These compounds exhibit diverse pharmacological properties and find applications in drug discovery and development.