Ring closing metathesis strategies to isoxazole containing thiadiazepines

Cyclic sulfamides are attractive molecules with potential application in medical chemistry. It is known that thiadiazepine-containing derivatives demonstrate promising value in the development of protease inhibitors such as HIV protease, serine protease and metaloprotease. We demonstrate here a comfortable synthetic sequence to symmetric thiadiazepines containing isoxazole substitutents. The structure of the obtained substances was confirmed by 1H, 13C NMR spectroscopy.

Asymmetric Synthesis of Six-Membered Cyclic Sulfamides via Palladium-Catalyzed Alkene Carboamination Reactions

The asymmetric synthesis of six-membered cyclic sulfamides via palladium-catalyzed alkene carboamination reactions of N-homo­allylsulfamides with aryl halides is described. High levels of enantio­selectivity were obtained with a catalyst composed of Pd2dba3 and (S)-Siphos-PE.

Intramolecular 1,5-C(sp3)–H radical amination via Co(ii)-based metalloradical catalysis for five-membered cyclic sulfamides

Synthesis of strained five-membered cyclic sulfamides has been achieved for the first time by intramolecular 1,5-C(sp3)–H aminationviaCo(ii)-based metalloradical catalysis.