Abstract: Multicomponent reactions (MCRs) are very powerful methods for the total synthesis of natural products, drugs, biologically active molecules in one-pot fashion, starting from more than two commercially available starting materials.1,2 The four component reaction of isocyanides, primary amines, aldehydes/ketones with carboxylic acids invented by Iver Ugi is considered to be one of the most important reaction among the isocyanide-based MCRs.3,4 Attempts have been made by several research groups for uncovering the enantioselective version of the Ugi reaction for many years.5-9 Recently, Tan, Houk and co-workers have developed an efficient method for the catalytic enantioselective U-4CR using chiral phosphoric acid (CPA) derivative as the catalyst.10 These details will be presented.
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