Current medicinal chemistry relies heavily on the quality of building blocks, ie reagents used
to introduce chemical diversity into the target molecules. The last decade witnessed an …

Applications of piperazine and homopiperazine in drug design are well-established, and
these heterocycles have found use as both scaffolding and terminal elements and also as a …

Achieving single-step syntheses of a set of related compounds divergently and selectively
from a common starting material affords substantial efficiency gains when compared with …

Natural products like coumarins, chalcones, and resveratrol have inherent biological activity
in several models of diseases; therefore, their natural dimeric forms are highlighted in this …

Electrophilic double bond functionalization–intramolecular enolate alkylation sequence was
used to obtain a series of bridged and fused bicyclo [mnk] alkane derivatives (ie, bicyclo [4.1 …

The term “conformational restriction” can be found very often in contemporary chemical
literature. Despite the lack of strict definitions, this term is usually intuitively understood and …

The 2‐substituted piperidine core is found in drugs (18 FDA‐approved drugs), however,
their spirocyclic analogues remain unknown. Described here is the synthesis of spirocyclic …

DNA-encoded library (DEL) screens have significantly impacted new lead compound
identification efforts within drug discovery. An advantage of DELs compared to traditional …

The synthesis of multifunctional spirocycles was achieved from common cyclic carboxylic
acids (cyclobutane carboxylate, cyclopentane carboxylate, l‐proline, etc.). The whole …

The synthesis of 3-azabicyclo [3.2. 0] heptyl boropinacolates and trifluoroborates via the [2+
2] photocycloaddition of the corresponding alkenyl boronic derivatives and maleimides or …