1-Bromo-4-(S-methylsulfonimidoyl)benzene (BD336512) is a building block containing a sulfoximine group. Several CDK and ATR inhibitors have exemplified the utilization of the NH sulfoximine group as abioisostere for a sulfonamide group to overcome the main project hurdles of aqueous solubility, sulfonamide-mediated off-target activity and IP. Moreover, its NH group could be expediently further functionalized through Buchwald-Hartwig coupling reaction and multifarious nucleophilic reactions.. Recommended Products is: 4381-25-3 and 83730-53-4.
A method for the synthesis of a large number of 1,2-benzothiazines I (3a-u; R1 = H, Me, Me2, Cl, Br, OMe; R2 = Me, Et, iPr, cyclopropyl, C6H13, Ph; R3 = H, Me, X = Cl, Br) bearing pyridyl as well as carbonyl groups is developed from rhodium-catalyzed carbene insertions into aromatic C-H bonds of S-aryl sulfoximines R1C6H4SO(R2)NH using [1,2,3]triazolo[1,5-a]pyridines (H3tzp) 3-(EtO2C)-7-X-R1tzp by denitrogenative cyclization followed by the elimination of alcs. and dinitrogen. The present method involves the N-H/C-H activation of simple alkyl aryl sulfoximines and has the advantages of a broad substrate scope, high functional group tolerance, and good regioselectivity.
Synthesis of 1,2-benzothiazines by a rhodium-catalyzed domino C-H activation/cyclization/elimination process from S-aryl sulfoximines and pyridotriazoles. Recommended basis is Sulfoximine, Bioisosteric. Products is: https://www.ambeed.com/products/1621962-30-8.html, 50578-18-2
Referemce:
Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem