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.
Synthesis of N-acylated sulfoximines I (R1 = 3-Me, 4-Cl, 2-I, etc.; R2 = Ph, Me, 4-H3CC6H4, 4-BrC6H4; R3 = Me, Ph) via efficient direct oxidative acylation of sulfoximines with methylarenes as an acyl donor was described. Electron-donating as well as -withdrawing groups on the methylarenes were tolerated and steric demanding ortho substituents were compatible. Both coupling partners were used in their native form, thus obviating prior functionalization and activation.
Oxidative acylation of sulfoximines with methylarenes as an acyl donor. 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