One-Step, Catalyst-Free\nContinuous-Flow Method for\nthe Rapid and Safe Synthesis of 1‑Substituted 1<i>H</i>‑Tetrazoles

1-Substituted 1<i>H</i>-tetrazoles are valuable\nbuilding\nblocks in medicinal chemistry; however, their limited synthetic accessibility\nconstrains their use. A new continuous-flow strategy was developed\nto safely obtain tetrazoles from primary amines within minutes. Method\noptimization was aided by theoretical studies leading to different\nconditions depending on the amine structure. The versatility of our\nmethod was demonstrated by using a set of benzylic, aromatic, aliphatic,\nand heteroaromatic amines leading to previously unexplored tetrazoles\nwith satisfactory yields.

Publication Details

Journal
Figshare
Published
2024-09-05
DOI
https://doi.org/10.1021/acs.oprd.4c00239.s001
Primary Topic
Wheat and Barley Genetics and Pathology
Type
article
Field-Weighted Citation Impact
0.00
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article

One-Step, Catalyst-Free\nContinuous-Flow Method for\nthe Rapid and Safe Synthesis of 1‑Substituted 1H‑Tetrazoles

Figshare
Wheat and Barley Genetics and Pathology
article

One-Step, Catalyst-Free\nContinuous-Flow Method for\nthe Rapid and Safe Synthesis of 1‑Substituted 1H‑Tetrazoles

article en

Abstract

1-Substituted 1<i>H</i>-tetrazoles are valuable\nbuilding\nblocks in medicinal chemistry; however, their limited synthetic accessibility\nconstrains their use. A new continuous-flow strategy was developed\nto safely obtain tetrazoles from primary amines within minutes. Method\noptimization was aided by theoretical studies leading to different\nconditions depending on the amine structure. The versatility of our\nmethod was demonstrated by using a set of benzylic, aromatic, aliphatic,\nand heteroaromatic amines leading to previously unexplored tetrazoles\nwith satisfactory yields.

Figshare
Openalex Percentile: Top 40%
Wheat and Barley Genetics and Pathology
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One-Step, Catalyst-Free\nContinuous-Flow Method for\nthe Rapid and Safe Synthesis of 1‑Substituted 1<i>H</i>‑Tetrazoles · Figshare (2024) | TGRS Research Map | TGRS