1-Iminotetrahydrothiophene 1-oxide (BD00963737) 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 solution of sodium anthracenide in DME was added dropwise to a stirred solution or suspension of N-tosylsulfoximes RR1S(O):NTs [I; Ts = tosyl, R = R1 = Me, Bu; R = Me, R1 = morpholino, Bu2N; RR1 = (CH2)4] in DMF under argon at 0¡ã to afford 68-98% sulfoximines RR1S(O):NH. I (R = Et, R1 = MeCCl2) gave S,S-diethylsulfoximine; I (R = Me, R1 = Ph, PhCH2) were unreactive.
Preparation of free sulfoximines by treatment of N-tosylsulfoximines with sodium anthracenide. Recommended basis is Sulfoximine, Bioisosteric. Products is: https://www.ambeed.com/products/1621962-30-8.html, 145026-07-9
Referemce:
Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem