Synthesis of the Energetic Material 4-Nitro-3,5-bis(trinitromethyl)-1 H -pyrazole through Two Synthetic Strategies

4‑Nitro‑3,5‑bis(trinitromethyl)‑1H‑pyrazole (1) is an intriguing and highly substituted polynitro pyrazole featuring two symmetric trinitromethyl groups and a 4‑nitro‑functionalized pyrazole core, which poses a formidable challenge for its concise synthesis. Herein, we describe the development of two complementary synthetic strategies toward compound 1. The symmetric trinitromethyl moieties are efficiently installed via nucleophilic substitution followed by a two‑step nitration sequence, starting from commercially available 3,6‑dichloro‑1,2,4,5‑tetrazine (13). Initially, a Knorr pyrazole approach was developed starting from commercially available ethyl acetoacetate; although the pyrazole ring could be efficiently constructed using hydrazine acetate, this route suffers from a relatively long synthetic sequence and low overall yield. Alternatively, a [4 + 1] cycloaddition strategy was investigated, which delivered the 4‑aminopyrazole intermediate in a single step. Subsequent oxidation of the amino group, followed by a high‑yielding nitration, successfully generated the 4‑nitropyrazole scaffold and enabled the highly efficient synthesis of 1 in only 5 steps.

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Publication Details

Journal
The Journal of Organic Chemistry
Published
2026-11-06
DOI
https://doi.org/10.1021/acs.joc.6c02263
Primary Topic
Energetic Materials and Combustion
Type
article
Field-Weighted Citation Impact
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article

Synthesis of the Energetic Material 4-Nitro-3,5-bis(trinitromethyl)-1 H -pyrazole through Two Synthetic Strategies

Linyuan Wen, Wentong Tu, Yingzhe Liu, Qiurong Li et al.
1 links
The Journal of Organic Chemistry
Energetic Materials and Combustion
article

Synthesis of the Energetic Material 4-Nitro-3,5-bis(trinitromethyl)-1 H -pyrazole through Two Synthetic Strategies

Linyuan Wen, Wentong Tu, Yingzhe Liu, Qiurong Li, Hongyao Xu, Jinjun Wang, Qianqian He, Tao Yu
article en

Abstract

4‑Nitro‑3,5‑bis(trinitromethyl)‑1H‑pyrazole (1) is an intriguing and highly substituted polynitro pyrazole featuring two symmetric trinitromethyl groups and a 4‑nitro‑functionalized pyrazole core, which poses a formidable challenge for its concise synthesis. Herein, we describe the development of two complementary synthetic strategies toward compound 1. The symmetric trinitromethyl moieties are efficiently installed via nucleophilic substitution followed by a two‑step nitration sequence, starting from commercially available 3,6‑dichloro‑1,2,4,5‑tetrazine (13). Initially, a Knorr pyrazole approach was developed starting from commercially available ethyl acetoacetate; although the pyrazole ring could be efficiently constructed using hydrazine acetate, this route suffers from a relatively long synthetic sequence and low overall yield. Alternatively, a [4 + 1] cycloaddition strategy was investigated, which delivered the 4‑aminopyrazole intermediate in a single step. Subsequent oxidation of the amino group, followed by a high‑yielding nitration, successfully generated the 4‑nitropyrazole scaffold and enabled the highly efficient synthesis of 1 in only 5 steps.

The Journal of Organic Chemistry
Fuyang University of Technology (CN)
National Natural Science Foundation of China, Natural Science Foundation of Shaanxi Province, University Natural Science Research Project of Anhui Province, National College Students Innovation and Entrepreneurship Training Program
Openalex Percentile: Top 32%
Energetic Materials and Combustion
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