7-Bromo-4-chloro-1H-indazol-3-amine is a heterocyclic fragment used in the synthesis of Lenacapavir, a potent capsid inhibitor for the treatment of HIV-1 infections. In this manuscript, we describe a new approach to synthesizing 7-bromo-4-chloro-1H-indazol-3-amine from inexpensive 2,6-dichlorobenzonitrile. This synthetic method utilizes a two-step sequence including regioselective bromination and heterocycle formation with hydrazine to give the desired product in an overall isolated yield of 38–45%. The new protocol has been successfully demonstrated on hundred-gram scales without the need for column chromatography purification. This new synthesis provides a potential economical route to the large-scale production of this heterocyclic fragment of Lenacapavir.

中文翻译：

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7-溴-4-氯-1H-吲唑-3-胺的实际合成：来那卡韦的重要中间体


7-Bromo-4-氯-1H-indazol-3-amine 是一种杂环片段，用于合成 Lenacapavir，Lenacapavir 是一种有效的衣壳抑制剂，用于治疗 HIV-1 感染。在这篇手稿中，我们描述了一种从廉价的 2,6-二氯苯甲腈合成 7-溴-4-氯-1H-吲唑-3-胺的新方法。该合成方法采用两步序列，包括区域选择性溴化和与肼形成杂环，以 38-45% 的总分离产率得到所需产物。新方案已在百克规模上成功论证，无需柱层析纯化。这种新的合成方法为大规模生产 Lenacapavir 杂环片段提供了一条潜在的经济途径。