Related Experiment Video
Updated: Jun 1, 2026

Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay
Published on: February 9, 2021
Systematic enumeration of heteroaromatic ring systems as reagents for use in medicinal chemistry
Richard A Ward1, Jason G Kettle
1Oncology iMED, AstraZeneca, Mereside, Alderley Park, Macclesfield, UK. Richard.A.Ward@AstraZeneca.com
Abstract:
The availability of suitable chemical building blocks, or reagents, is a key factor that determines the degree of effort required to make a target molecule. If a reagent is not available and requires synthesizing, this increases the total number of synthetic steps in the route and may result in a less attractive synthetic target. This can impact most in compound collection enhancement activities or early lead identification (LI) where typically not enough information or data are available to commit to such long multistep syntheses. In lead optimization (LO) projects, having access to commonly used reagents may improve the efficiency of building structure-activity relationships (SARs) and structure-property relationships (SPRs) around a core scaffold. This paper describes the systematic enumeration of key heteroaromatic reagent classes and the subsequent analysis of the availability of these in a number of commonly used databases.
More Related Videos
Related Concept Videos
Nomenclature of Aryl and Heterocyclic Amines
Five-Membered Heterocyclic Aromatic Compounds: Overview
ortho–para-Directing Activators: –CH3, –OH, –⁠NH2, –OCH3
Aromatic Compounds: Overview
In 1825, Faraday isolated benzene...
Basicity of Heterocyclic Aromatic Amines
Nucleophilic Aromatic Substitution of Aryldiazonium Salts: Aromatic SN1
In the Sandmeyer reaction, for example, the diazonio group is replaced by a chloro, bromo, or cyano...

