Chemical Science · 2024 · 17 citations · 30 references
PharmacyChemistryMedicinal ChemistryDrug DiscoveryStructure-activity RelationshipsSynthetic Medicinal ChemistryCross-coupling ReactionsTarget-oriented SynthesisAllylic FunctionalizationCoupling Reagent ChemistryMedicinal Chemistry ApplicationsReaction Selectivity EngineeringSelectivity
a Pd(ii)/Pd(0) reaction modality resulted in geminal selectivity. The protocol is operationally simple, scalable, and offers two distinct types of products bearing functionalized tryptamine and bisindolyl frameworks in very high to excellent yields. The reaction features a wide substrate generality and also remains effective in the presence of various medicinally relevant scaffolds. Notably, this work represents the first example of nucleopalladation-guided intermolecular dicarbofunctionalization of allylamines.
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