Reductive Amination in the Synthesis of Pharmaceuticals.,Chemical Reviews

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Reductive Amination in the Synthesis of Pharmaceuticals.
Chemical Reviews ( IF 51.4 ) Pub Date : 2019-10-21 , DOI: 10.1021/acs.chemrev.9b00383
Oleg I Afanasyev ₁ , Ekaterina Kuchuk ₁ , Dmitry L Usanov ₂ , Denis Chusov _{1,

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Affiliation

Reductive amination plays a paramount role in pharmaceutical and medicinal chemistry owing to its synthetic merits and the ubiquitous presence of amines among biologically active compounds. It is one of the key approaches to C-N bond construction due to its operational easiness and a wide toolbox of protocols. Recent studies show that at least a quarter of C-N bond-forming reactions in the pharmaceutical industry are performed via reductive amination. This Review concisely compiles information on 71 medical substances that are synthesized by reductive amination. Compounds are grouped according to the principle of action, which includes drugs affecting the central nervous system, drugs affecting the cardiovascular system, anticancer drugs, antibiotics, antiviral and antifungal medicines, drugs affecting the urinary system, drugs affecting the respiratory system, antidiabetic medications, drugs affecting the gastrointestinal tract, and drugs regulating metabolic processes. A general synthetic scheme is provided for each compound, and the description is focused on reductive amination steps. The green chemistry metric of reaction mass efficiency was calculated for all reactions.

中文翻译：

药物合成中的还原胺化。

还原胺化由于其合成优点和在生物活性化合物中普遍存在的胺类，在药物和药物化学中起着至关重要的作用。由于其操作简便性和广泛的协议工具，它是构建CN键的关键方法之一。最近的研究表明，制药行业中至少四分之一的CN键形成反应是通过还原胺化进行的。该评论简明扼要地汇编了通过还原胺化合成的71种药物的信息。根据作用原理将化合物分类，包括影响中枢神经系统的药物，影响心血管系统的药物，抗癌药物，抗生素，抗病毒和抗真菌药物，影响泌尿系统的药物，影响呼吸系统的药物，抗糖尿病药物，影响胃肠道的药物以及调节代谢过程的药物。提供了每种化合物的一般合成方案，其描述集中于还原胺化步骤。计算所有反应的反应质量效率的绿色化学度量。

更新日期：2019-10-21

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