Spirocyclic scaffolds are incorporated in various approved drugs and drug candidates. The
increasing interest in less planar bioactive compounds has given rise to the development of …

Aliphatic three-and four-membered rings including cyclopropanes, cyclobutanes, oxetanes,
azetidines and bicyclo [1.1. 1] pentanes have been increasingly exploited in medicinal …

Cyclobutanes are increasingly used in medicinal chemistry in the search for relevant
biological properties. Important characteristics of the cyclobutane ring include its unique …

Spirocycles are ring systems in which two rings are fused through a single atom, referred to
as the spiro atom. The ethylene glycol ketal of cyclohexanone is an example of a well-known …

An analysis of 66 published clinical candidates from Journal of Medicinal Chemistry has
been conducted to shed light on which lead generation strategies are most frequently …

Two catalytic systems have been developed for the arylboration of endocyclic
enecarbamates to deliver synthetically versatile borylated saturated N‐heterocycles in good …

Drug discovery and development is a complex and lengthy enterprise that suffers from high
rates of candidate attrition at all stages of the process. The physical, biological, and …

We consider the conformational flexibility of molecules and its implications for micro-and
macro-p K a. The corresponding formulas are derived and discussed against the …

The compact and versatile oxetane motifs have gained significant attention in drug discovery
and medicinal chemistry programs. This review presents an overview of the diverse …

The use of flow technology as an enabling tool for accessing 1-azabicyclo [1.1. 0] butanes
bearing strained 3-, 4-, and 5-membered O-heterocycles with C3 (N-het)–C2 (O-het) …