Dolutegravir (DTG), Bictegravir (BIC), and Cabotegravir (CAB) are the second-generation integrase strand transfer inhibitors (INSTIs) that have been FDA-approved for the treatment of HIV-1 infection. Preparation of these INSTIs utilizes the common intermediate 1-(2,2-dimethoxyethyl)-5-methoxy-6-(methoxycarbonyl)-4-oxo-1,4-dihydropyridine-3-carboxylic acid (6). Presented herein is a literature and patent review of synthetic routes used to access the pharmaceutically important intermediate 6. The review highlights the ways in which small fine-tuned synthetic modifications have been used to achieve good yields and regioselectivity of ester hydrolysis.

中文翻译：

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HIV-1 整合酶链转移抑制剂 Dolutegravir、Bictegravir 和 Cabotegravir 常见的关键吡啶酮羧酸前体的合成方法

Dolutegravir (DTG)、Bictegravir (BIC) 和 Cabotegravir (CAB) 是第二代整合酶链转移抑制剂 (INSTI)，已获 FDA 批准用于治疗 HIV-1 感染。这些 INSTI 的制备使用了常见的中间体 1-(2,2-二甲氧基乙基)-5-甲氧基-6-(甲氧基羰基)-4-氧代-1,4-二氢吡啶-3-羧酸 (6 )。本文介绍的是用于获取药学上重要的中间体6的合成路线的文献和专利综述。该综述强调了使用微调合成修饰来实现酯水解的良好产率和区域选择性的方法。