Stable isotopes have become vital tools in drug development and discovery. Because of the unique high neutron absorption properties of boron-10, boron neutron capture therapy (BNCT) has been considered as an ideal technology for cancer treatment. Along with the promising progress of accelerator neutron sources, the efficient synthesis of ¹⁰B-enriched molecular carriers becomes crucial for BNCT drug development. However, there is a lack of enriched ¹⁰B-reagent available for installing ¹⁰B in various carriers. Herein, we developed a synthesis of ¹⁰B-enriched diboron(4) reagents from the primary source of boron-10, ¹⁰BF₃. The conversion of BF₃ to chloro-diaminoboron in the presence of chlorosilane and diamine is crucial for its success. The synthesis of these diboron(4) reagents will not only build up an efficient bridge between inorganic ¹⁰B-source and numerous organic ¹⁰B-molecules but also benefit boron-related mechanistic studies. The use of ¹⁰B₂pin₂ in several catalytic borylation technologies produces various organo-¹⁰B compounds, including the approved BNCT drug ¹⁰B-L-BPA.

稳定同位素已成为药物开发和发现的重要工具。由于硼10独特的高中子吸收特性，硼中子俘获疗法（BNCT）被认为是癌症治疗的理想技术。随着加速器中子源的不断取得进展，^10B富集分子载体的有效合成对于BNCT药物开发变得至关重要。然而，缺乏可用于在各种载体中安装^{10 B 的富集10} B 试剂。在此，我们开发了一种从硼-10、¹⁰ BF _{3的主要来源合成}¹⁰ B富集二硼(4)试剂的方法。 在氯硅烷和二胺存在下， BF ₃转化为氯代二氨基硼对于其成功至关重要。^{这些二硼(4)试剂的合成不仅将在无机10} B 源和众多有机¹⁰ B 分子之间建立有效的桥梁，而且有利于硼相关的机理研究。在多种催化硼化技术中使用¹⁰ B ₂ pin ₂可产生各种有机¹⁰ B 化合物，包括批准的 BNCT 药物¹⁰ B-L-BPA。