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.
An iron-catalyzed dealkylative acylation of N-alkylsulfoximines RN=S(O)R1R2 [R = CH3, CH3(CH2)3, (CH2)9CH=CH, etc.; R1 = CH3, C6H5, 4-ClC6H4, 4-BrC6H4, 4-H3COC6H4; R2 = CH3, C6H5, c-C3H5; R1R2 = -(CH2)4-] has been developed. This process involves a Polonovski-type dealkylation of an N-alkylated sulfoximine to afford a reactive intermediate that is trapped in the presence of a suitable aldehyde R3CHO (R3 = C6H5, 2-H3CC6H4, 3-ClC6H4, etc.) or anhydride R4C(O)OC(O)R4 [R = CH3, CH3(CH2)4, C6H5CH=CH, etc.] to afford N-acylsulfoximine derivatives R1R2S(O)=NR4 and N-aroylsulfoximine derivatives R1R2S(O)=NR3 in one pot. Subsequent cleavage of the acyl or aroyl group under acidic conditions generates a synthetically valuable NH-sulfoximines R1R2S(O)=NH.
Iron-Catalyzed Acylative Dealkylation of N-Alkylsulfoximines. 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