Retrosynthetic Simplicity

Abstract

Retrosynthetic simplicity is introduced as a metric by which methods can be evaluated. An argument in favor of reactions which are retrosynthetically simple is put forward, and recent examples in the context of skeletal editing from my own laboratory as well as contributions from others are analyzed critically through this lens.

1 Introduction

2 Example 1: Quinoline to Quinazoline (One Product, Two Starting Materials)

3 Example 2: Benzene to Pyridine (Two Products, One Starting ­Material)

4 Caveats, Counterarguments, and Conclusions

Key words

skeletal editing - retrosynthesis - simplicity - heterocycles - methodology

Publication History

Received: 08 October 2023

Accepted after revision: 06 November 2023

Article published online:
09 November 2023

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