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 metal-free, iodine-catalyzed N-H/S-H dehydrocoupling reaction of sulfoximines R1S(O)(R2)=NH (R1 = Ph, 4-CH3OC6H4, 4-ClC6H4, etc.; R2 = Ph, Me, cyclopropyl, etc.) and anilines R4C6H4NHR5 (R4 = H, 4-Me, 4-Br, 4-C(O)OCH3, etc.; R5 = H, Me) with various thiols R3SH (R3 = 3-CH3C6H4, pyridin-2-yl, 1,3-benzothiazol-2-yl, etc.) to construct sulfur-nitrogen bonds is herein presented. A variety of structurally diverse N-sulfenylsulfoximines R1S(O)(R2)=NSR3 and sulfenamides R4C6H4N(R5)SC6H5 was prepared with up to 97% yield. The reaction was carried out in the presence of hydrogen peroxide in PEG400 under mild conditions.
Synthesis of N-sulfenyl-sulfoximines and -sulfenamides through a metal-free N-H/S-H dehydrocoupling reaction. 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