Synthesis of N–BOH Benzazaborines via a Modular GBB-Based Strategy

A green, one-pot Groebke-Blackburn-Bienaymé reaction is reported for the efficient synthesis of N-BOH benzazaborines. The products precipitate directly from methanol, enabling purification by simple filtration without chromatography. This scalable, operationally simple method uniquely combines synthetic efficiency with environmental sustainability, providing rapid access to boron-nitrogen scaffolds for medicinal chemistry.

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Publication Details

Journal
Organic Letters
Published
2026-06-29
DOI
https://doi.org/10.1021/acs.orglett.6c02007
Primary Topic
Organoboron and organosilicon chemistry
Type
article
Field-Weighted Citation Impact
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article

Synthesis of N–BOH Benzazaborines via a Modular GBB-Based Strategy

Zhigang Xu, Shi-Yu Xue, Jian-Jun Cheng, Tian Tan et al.
Organic Letters
Organoboron and organosilicon chemistry
article

Synthesis of N–BOH Benzazaborines via a Modular GBB-Based Strategy

Zhigang Xu, Shi-Yu Xue, Jian-Jun Cheng, Tian Tan, Zhe-Xuan Li, Xue Li, Yi-Ming Chen, Chen-Hui Cao, Chuan Xu
article en

Abstract

A green, one-pot Groebke-Blackburn-Bienaymé reaction is reported for the efficient synthesis of N-BOH benzazaborines. The products precipitate directly from methanol, enabling purification by simple filtration without chromatography. This scalable, operationally simple method uniquely combines synthetic efficiency with environmental sustainability, providing rapid access to boron-nitrogen scaffolds for medicinal chemistry.

Organic Letters
Target (United States) (US), University of Electronic Science and Technology of China (CN), Chengdu Medical College (CN), Chongqing University of Arts and Sciences (CN), Sichuan Academy of Medical Sciences & Sichuan Provincial People's Hospital (CN), First Affiliated Hospital of Chengdu Medical College (CN)
Responsible consumption and production
Openalex Percentile: Top 13%
Organoboron and organosilicon chemistry
DOISourceOpenAlex
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Synthesis of N–BOH Benzazaborines via a Modular GBB-Based Strategy — Zhigang Xu, Shi-Yu Xue, et al. · Organic Letters (2026) | TGRS Research Map | TGRS