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 …

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 …

A general approach to dense substitution patterns via [2+ 2]/[2+ 3] cycloaddition between
nonstabilized azomethine ylides, alkynes and silyl enol ethers is elaborated. This approach …

A scalable and efficient process for the preparation of 3‐borylated pyrrolidines by 1, 3‐
dipolar cycloaddition of N‐benzyl azomethine ylide generated in situ has been developed …

Propellanes and derivatives have attractive properties due to their unique structure.
Therefore,[3.3. 3] propellanes, containing tricyclic structures with one of the carbon-carbon …

The generated databases (GDBs) enumerate billions of possible molecules following simple
rules of chemical stability and synthetic feasibility. Exploring the GDBs shows that many …

Abstract Scalable [3+ 2] cycloaddition of alkynyl boronates and in situ generated
unstabilized azomethine ylide is reported for the first time. The selective formation of either 1 …

A protocol for the multigram synthesis of 3-substituted 2, 5-dihydro-1 H-pyrrole boronic
derivatives is reported. The method relied on the triflation of N-Boc-3-oxopyrrolidine and …

Here we searched chemical space for small and novel diamond‐like, 3D‐shaped building
blocks, which are very rare but highly valuable for medicinal chemistry because they can …

One‐pot intramolecular cyclization of novel sp3‐enriched cyanoalkylsulfonyl fluorides into
spirocyclic β‐or γ‐sultams is disclosed. The method relies on nitrile group reduction followed …