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 one-pot Michael addition/cyclization/condensation reaction sequence for the regioselective synthesis of 1,2-thiazines I (R1 = C6H5, 4-BrC6H4, CH3, 4-H3COC6 H4; R2 = C6H5, 4-H3CC6H4, 3-H3CC6H4, 4-F3CC6H4, 2,5-(CH3)2C6H3; R3 = 4-H3COC6H4, C(CH3)3, thiophen-2-yl, 2-naphthyl, etc.; Y = O, C6H5NH2, N(CN), 4-H3COC6H4N), starting from propargyl ketones R2CCC(O)R3 and NH-sulfoximines or NH-sulfondiimines R1S(Y)(:NH)CH3, has been developed. Under mild and operationally simple reaction conditions previously unprecedented 1,2-thiazine 1-imide and 1-oxide derivatives I are formed in good to excellent yields. The products I represent heterocyclic building blocks, readily modifiable by a regioselective C-H bond functionalization, classical cross-coupling reactions, and deprotection.
1,2-Thiazines: One-Pot Syntheses Utilizing Mono and Diaza Analogs of Sulfones. 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