The discovery that oral administration of the oxazine dye, Nile blue A, to tumor-bearing mice resulted in diffuse staining of the tumor cells and significant retardation of their growth (1) led to the investigation of all available oxazine dyes. Further reports (2, 3) describe the action of a few of these dyes not only on transplanted sarcomata, but also on primary induced sarcomata and spon ta...

Oxazine derivatives are an important class of heterocycles, which has attracted much synthetic interest due to their wide range of biological activities. Oxazine is a heterocyclic compound can be formally derived from benzene, and its reduction products, by suitable substitution of carbon (and hydrogen) atoms by nitrogen and oxygen. In the last few years, oxazine derivatives have proved to be v...

Concise and stereocontrolled syntheses of (+)-hyacinthacine A2 and sphingofungin B were achieved via a diastereomerically enriched oxazine intermediate. The key strategies include palladium(0)-catalyzed intramolecular oxazine formation and diastereoselective nucleophilic addition to an aldehyde. (+)-Hyacinthacine A2 was synthesized in 13 steps and 10.2% overall yield and the synthesis of sphing...

A two step protocol is developed for the efficient synthesis of enantiopure N-Boc-dihydrobenzo[b]-1,4-oxazine-3-carboxylic acids 4 from serine derived cyclic sulfamidate via intramolecular arylamination. The RuPhos Palladacycle along with additional RuPhos ligand is found to be an efficient catalyst for the arylamination of β-(2-bromoaryloxy)amino acids 3 to provide easy and direct access to a ...

Iodination of carbohydrate-derived 3,6-dihydro-2H-1,2-oxazines of type 3 using iodine and pyridine in DMF furnished 5-iodo-substituted 1,2-oxazine derivatives 4 with high efficacy. The alkenyl iodide moiety of 1,2-oxazine derivatives syn-4 and anti-4 was subsequently exploited for the introduction of new functionalities at the C-5 position by applying palladium-catalyzed carbon-carbon bond-form...

Twenty-six benzocycloheptoxazine derivatives were investigated for their effect on nitric oxide (NO) production by lipopolysaccharide (LPS)-stimulated mouse macrophage-like RAW 264.7 cells. Benzo[b]cyclohepta[e][1,4]thiazine most effectively inhibited the LPS-stimulated NO production at noncytotoxic concentrations. 6H-Benzo[b]cyclohepta[e][1,4]-diazine cation, and benzo[b]cyclohepta[e][1,4]oxaz...

N-Substituted aminomethylphenol (Mannich base) and 3,4-dihydro-2H-3-substituted 1,3-benzoxazine (benzoxazine) were synthesized from substituted phenol (p-cresol, phenol, p-chlorophenol), substituted aniline (p-toluidine, aniline, p-chloroaniline) and formaldehyde to study influence of substituent on equilibrium of benzoxazine synthesis from Mannich base and formaldehyde. (1)H-NMR and charges of...

one of the most important goals in medicinal chemistry is the development of new techniques and new heterocyclic compounds with pharmaceutical activity. the present study aimed to use a method for the synthesis of some 1,2-dihydro-1-arylnaphtho [1,2-e] [1,3] oxazine-3-ones. the question this study tried to answer was this reaction can be performed in present of nano-fe2o3 as an acid catalyst an...

A novel method for oxazine derivatives formation is established using the reaction of ammonium thiocyanate and acid chlorides with 1-naphthol in the presence of Nanoparticle of ZnO to afford [1,3]oxazine-4-thione derivatives under solvent-free conditions at room temperature in excellent yields. 

In the title compound, C26H24N2O2, the oxazine moiety is fused to a naphthalene ring system. The asymmetric unit consists of one half of the mol-ecule, which lies about an inversion centre. The C atoms of the ethyl-ene spacer group adopt an anti-periplanar arrangement. The oxazine ring adopts a half-chair conformation. In the crystal, supra-molecular chains running along the b axis are formed v...