Emerging Building Blocks for Medicinal Chemistry: Recent Synthetic Advances

Abstract 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 sp 3 ‐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 sp 3 ‐enriched benzene isosteres, bicyclic morpholine/piperidine/piperazine analogs, as well as gem ‐difluorinated cycloalkanes (as an example of emerging fluorinated motifs) are discussed.