One-Step, Catalyst-Free Continuous-Flow Method for the Rapid and Safe Synthesis of 1-Substituted 1<i>H</i>-Tetrazoles
1-Substituted 1H-tetrazoles are valuable building blocks in medicinal chemistry; however, their limited synthetic accessibility constrains their use. A new continuous-flow strategy was developed to safely obtain tetrazoles from primary amines within minutes. Method optimization was aided by theoretical studies leading to different conditions depending on the amine structure. The versatility of our method was demonstrated by using a set of benzylic, aromatic, aliphatic, and heteroaromatic amines leading to previously unexplored tetrazoles with satisfactory yields.
Authors
- István Greiner (ORCID: https://orcid.org/0000-0002-5336-2828)
- János Éles (ORCID: https://orcid.org/0000-0001-9185-1123)
- Zoltán Kazsu
- Péter Bana (ORCID: https://orcid.org/0000-0001-5792-5926)
- Zsolt Fülöp (ORCID: https://orcid.org/0000-0001-8423-1583)
- Zoltán Béni (ORCID: https://orcid.org/0000-0002-1275-4155)
- Júlia Barabás (ORCID: https://orcid.org/0000-0001-5671-7316)
- Márton Temesvári
Institutions
- Gedeon Richter (Hungary) (HU)
- Budapest University of Technology and Economics (HU)
Publication Details
- Journal
- Organic Process Research & Development
- Published
- 2024-09-05
- DOI
- https://doi.org/10.1021/acs.oprd.4c00239
- Citations
- 3
- Primary Topic
- Innovative Microfluidic and Catalytic Techniques Innovation
- Type
- article
- Field-Weighted Citation Impact
- 0.55
Funders
- Richter Gedeon Talentum Alapítvány
- Nemzeti Kutatási, Fejlesztési és Innovaciós Alap