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.
An efficient catalytic method has been developed for the synthesis of N-aroylated sulfoximines ArC(O)N=S(O)R1R2 (Ar = C6H5, 3-H3COC6H4, naphthalen-1-yl, etc.; R1 = C6H5, 4-BrC6H4, 3-O2NC6H4, etc.; R2 = CH3, CH2CH3) from readily available toluenes (methylarenes) ArCH3 as source of the aroyl coupling partner and NH-sulfoximines NHS(O)R1R2, employing an environmentally benign iron catalyst. This protocol involves oxidation of benzylic C-H bonds of toluenes to generate aroyl radical intermediates followed by oxidative coupling with NH-sulfoximines to form N-aroylated sulfoximines in good to excellent yields. The intermediate aroyl radical is successfully trapped with TEMPO to prove the radical pathway of the reaction.
Iron-Catalyzed One-Pot N-Aroylation of NH-Sulfoximines with Methylarenes through Benzylic C-H Bond Oxidation. 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