A new Brønsted acid-catalyzed oxo-cyclization of propargyl alcohols with azlactones to synthesize C 2 -azlactonized 2H-chromenes has been established that uses 1,1′-binaphthyl-2,2′diyl hydrogen phosphate (BiNPO 4 H) as the catalyst and gives excellent diastereoselectivities (≥19:1 dr) in most cases. This protocol has a high compatibility with various substituents of substrates, offering a catalytic and useful entry to the fabrication of the synthetically important C 2 -functionalized 2H-chromene scaffold.α-Substituted 2H-chromenes and their analogs represent a valuable class of privileged oxo-containing heterocycles that are frequently encountered in a wide assortment of natural products, such as gaudichaudianic acid 1 and (+)-myristinin A, 2 and synthetic pharmaceuticals demonstrating antipsychotic, antibacterial, antifungal, antiviral, anticancer, antioxidative, antidepressive, antihypertensive, and antidiabetic activities (Figure 1). 3,4 Moreover, 2H-chromene derivatives

A new gold(I) self-relay catalysis enabling the annulative oxygenation of propargylic alcohols with various O-nucleophiles, such as carboxylic acids, alcohols and TBHP, is reported, producing a series of functionalized benzofurans...