Efficient Azacycle Formations Developed in Japanese Pharmaceutical Industries: Elegancy, Logistics, and Training (ELT) “Sandwich” for Process Chemists

Abstract

Efficient azacycle (nitrogen-containing heterocycle) formations developed by chemists in Japanese pharmaceutical industries have been selected from the published articles since the year 2000. The selected examples have been classified by the nitrogen source in the raw materials and have been reviewed from the following process chemistry perspectives; elegancy to establish the active pharmaceutical ingredient synthetic processes, logistics to procure/transform the required raw materials, and training for process chemists to consider azacycle formations according to a systematic approach. This mini-review also focuses on the molecular diversity created by the azacycle formations.

Chemoselective Reactions of Isocyanates with Secondary Amides: One-Pot Construction of 2,3-Dialkyl-Substituted Quinazolinones

“…Nitrogen-containing heterocycles are the most common structural architectures in natural products and find applications in the pharmaceutical and agricultural industries because of their wide spectrum of biological activities . Among them, quinazolinones are an important class of fused nitrogen heterocyclic compound that are found in many naturally occurring alkaloids and bioactive molecules .…”