The exploration of the complex chemical diversity of bicyclo [n. 1.1] alkanes and their use as
benzene bioisosteres has garnered significant attention over the past two decades …

The direct construction of bioisosteric compounds enriched in Csp3 content represents an
attractive and dependable approach to imbuing biologically active molecules with enhanced …

Synthesis of bicyclic scaffolds has gained significant attention in drug discovery due to their
potential to mimic benzene bioisosteres. Here, we present a mild and scalable Sc (OTf) 3 …

Bicyclo [1.1. 0] butanes, as structurally unique compounds with high strained energy and
diverse chemical properties, are becoming increasingly popular building blocks in organic …

While cycloaddition reactions of bicyclobutanes (BCBs) have emerged as a potent method
for synthesizing (hetero-) bicyclo [n. 1.1] alkanes (usually n≤ 3), their utilization in the …

We report the discovery of an example of oxidative bicyclo [1.1. 0] butane activation. This
reactivity stands in contrast to well-established strain-release nucleophile addition and …

Replacing planar aromatic rings in drug molecules with C (sp 3)-rich isosteric mimetics, such
as bicyclo [n. 1.1] alkanes, can significantly alter their physicochemical and pharmacokinetic …

Achieving structural and stereogenic diversity from the same starting materials remains a
fundamental challenge in organic synthesis, requiring precise control over the selectivity …

Within a medicinal chemist's toolbox, one of the most effective strategies to improve the
overall properties of a biologically active compound is bioisosteric replacement. Ever since …

Abstract Cycloaddition reactions of bicyclo [1.1. 0] butanes (BCBs) with 2 π components are
a powerful tool for preparing C (sp 3)-rich arene bioisosteres. Despite enormous progress in …