Application of sulfoximines in medicinal chemistry from 2013 to 2020

Pd‐Catalyzed Cascade Heck‐Type Annulation And Carbonylation to β‐Oxindolysulfoximidoyl Amides at Room Temperature

“…For example, some typical sulfoximine‐containing molecules, such as Suloxifen from Gödecke GmbH, [3] pan‐CDK inhibitor Roniciclib (BAY 1000394) from Bayer, [4] and AZD6738 from AstraZeneca, have found important medicinal applications in practical areas [5] . To date, numerous applications of the sulfoximine derivatives have been demonstrated in certain critical areas, such as medicinal developments, [2d,6] asymmetric catalysis, [7] crop protections, [8] and material sciences [9] …”

Synthesis of Enantiopure Benzo Fused Cyclic Sulfoximines Through Stereoselective [3+2] Cycloaddition between N‐tert‐Butanesulfinyl [(2‐Pyridyl)sulfonyl]‐difluoromethyl Ketimines and Arynes

“…Sulfoximines, as monoaza analogues of sulfones, have played multiple roles in organic chemistry, agricultural chemistry and medicinal chemistry since their initial discovery in 1940s [1–10] . In agricultural chemistry and medicinal chemistry, biologically active sulfoximines have been developed as pesticides [10] and drugs [5–9] . In organic chemistry, sulfoximines have been used as chiral auxiliaries and ligands as well as new reagents [2–4] .…”

Synthesis of chiral sulfinate esters by asymmetric condensation

“… Achiral sulfur functional groups, such as sulfonamide, sulfone, thiol and thioether, are common in drugs and natural products. By contrast, chiral sulfur functional groups are often neglected as pharmacophores 1 – 3 , although sulfoximine, with its unique physicochemical and pharmacokinetic properties 4 , 5 , has been recently incorporated into several clinical candidates. Thus, other sulfur stereogenic centres, such as sulfinate ester, sulfinamide, sulfonimidate ester and sulfonimidamide, have started to attract attention.…”