Affiliation:
1. Nantes Université CNRS BP 92208 F-44000 Nantes France
2. Janssen Research & Development Turnhoutseweg 30 2340 Beerse Belgium
3. NovAliX on-site Janssen-Cilag Centre de recherche Pharma Campus de Maigremont BP615 F-27106 Val de Reuil Cedex France
Abstract
AbstractThe pace and the scope of new molecules design is often constrained by limitations in synthetic chemistry. The azaheterocyclic amidrazones are of particular interest for bioisosteric considerations in drug discovery. However, the lack of efficient synthetic access has undoubtedly hampered their occurrence in the drug chemical space. Our current results describe a robust synthetic access relying on cyclization of aminohydrazine in presence of various orthoesters by either metal free‐ or metal‐catalyzed condensations. This optimized synthetic access to cyclic amidrazones as original scaffold should inspire the chemist community and further drive innovation in the design of molecular structure for many applications (for example, drugs, materials, dyes).
Subject
Organic Chemistry,Physical and Theoretical Chemistry