The oxetane ring is an emergent, underexplored motif in drug discovery that shows attractive
properties such as low molecular weight, high polarity, and marked three-dimensionality …

An oxetane can trigger profound changes in aqueous solubility, lipophilicity, metabolic
stability, and conformational preference when replacing commonly employed functionalities …

The four-membered oxetane ring has been increasingly exploited for its contrasting
behaviors: its influence on physicochemical properties as a stable motif in medicinal …

In drug discovery, it is common practice to block metabolically exposed sites in a biologically
active molecule by the introduction of a gem-dimethyl unit (Figure 1). However, for a typical …

Sizable resources, both financial and human, are invested each year in the development of
new pharmaceutical agents. However, despite improved techniques, the new compounds …

We were intrigued by the apparent analogy between oxetanes and the van t Hoff description
of R2C= O,[1] with the close correspondence of these two structural types in the “bent-bond” …

Oxetanes are used in drug discovery to enable physicochemical and metabolic property
enhancement for the structures to which they are grafted. An imide C O to oxetane swap on …

Oxetanes are valuable intermediates in organic synthesis, and strategic manipulations of
this strained heterocycle continue to emerge. In this Synopsis, recent, distinct approaches to …

Four-membered rings are witnessing significant prominence in medicinal chemistry
discovery programs. For example, a search of the chemical databases shows exponential …

Bioisosteres provide valuable design elements that medicinal chemists can use to adjust the
structural and pharmacokinetic characteristics of bioactive compounds towards viable drug …