Future Stars Discovery Bay

It’s often said, "The past is prologue". In case of the future, it's safe to say time has yet to tell. Let's look at some of the future stars from around the world and forecast their future aspirations and likely success.

Discovery

The fickle summer weather took its toll on the ever-popular July Stableford Tournament, presented by bulthaup kitchen architecture, after it was cancelled due to persistent rainstorms that thundered above Discovery Bay Golf Club on July 19. Although some competitors were able to commence their rounds, conditions rapidly deteriorated and play was halted later in the morning. The event was sponsored by bulthaup, the leading German kitchen system manufacturer, which also hosted the June Stableford Tournament.

Sulfoximines have been largely disregarded in medicinal chemistry for a long time. However, recently, they have risen to the apparent level of stardom on the drug discovery scene. Considering the outstanding properties of sulfoximines, this versatile functional group has advanced to implementation in several drug discovery programs. Currently, this fashionable functional group can be found in various hit-to-lead and lead optimization studies in early stages and in several compounds currently in clinical trials. Herein, we review recent developments to demonstrate the scope and limitations of this interesting and versatile functional group in medicinal chemistry and drug discovery. (Source: www.researchgate.net)

Review

Current medicinal chemistry relies heavily on the quality of building blocks, i.e. reagents used to introduce chemical diversity into the target molecules. The last decade witnessed an emergence of many novel (or well‐overlooked old) chemotypes for drug discovery, which is related to adapting new synthetic methodologies, designing new sp3‐enriched bioisosteres, paying attention to previously underrated (or even unwanted) structural motifs, or combination thereof. In this review with 532 references, a survey of selected chemotypes that emerged recently in medicinal chemistry is provided, with a focus on the synthesis of the corresponding building blocks. Thus, saturated (hetero)aliphatic boronates, sulfonyl fluorides, sulfinates, non‐classical sp3‐enriched benzene isosteres, bicyclic morpholine/piperidine/piperazine analogs, as well as gem‐difluorinated cycloalkanes (as an example of emerging fluorinated motifs) are discussed.

Recent years have seen a marked increase in the occurrence of sulfoximines in the chemical sciences, often presented as valuable motifs for medicinal chemistry. This has been prompted by both pioneering works taking sulfoximines containing compounds into clinical trials and the concurrent development of powerful synthetic methods. This review covers recent developments in the synthesis of sulfoximines concentrating on developments since 2015. This includes extensive developments in both S‐N and S‐C bond formations. Flow chemistry processes for sulfoximine synthesis are also covered. Finally, subsequent transformations of sulfoximines, particularly in N‐functionalization are reviewed, including N–S, N–P, N–C bond forming processes and cyclization reactions. (Source: www.researchgate.net)