RuCl 2 (PPh 3 ) 3 -Catalyzed Facile One-Pot Synthesis of 1,2-Dihydro-1-arylnaphtho[1,2-e][1,3]oxazine-3-ones and 1,2-Dihydro-1-arylnaphtho[1,2-e][1,3]oxazine-3-thiones

Benzoxazinones and benzthioxazinones have received considerable attention because of the attractive pharmacological properties associated with their heterocyclic scaffold. Molecules bearing these skeletons have been reported to exhibit a variety of biological properties, including antiinflammatory, antiulcer, antipyretic, antihypertensive, and antifungal activities. Some of these compounds also exhibit several important biological activities such as DP receptor antagonism, integrin antagonism, platelet fibrinogen receptor antagonism, calmodulin antagonism, and inhibition of the transforming growth factor β (TGF-β) signaling pathway, soybean lipoxygenase, and other protein kinase. Because of the importance of these compounds, several synthetic methods for 1,2-dihydro-1-arylnaphtho[1,2-e][1,3]oxazine3-ones and 1,2-dihydro-1-arylnaphtho[1,2-e][1,3]oxazine-3thiones have been developed. The reported methods mainly include one-pot three-component reactions of 2naphthol, aromatic aldehydes, and urea or thiourea (Scheme 1). These reactions for the synthesis of 2-dihydro-1-arylnaphtho[1,2-e][1,3]oxazine-3-ones have been studied with the use of several catalysts and reagents such as Cu-nanoparticles/PEG-400, TMSCl, HClO4/SiO2, 12 H3Mo12O40P, 13

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