Streamlining drug synthesis

JOEL M. HAWKINS

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Streamlining drug synthesis

机译：简化药物合成

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The active ingredients of pharmaceuticals are typically structurally complex organic molecules that have precise arrangements of chemical groups. They are made using sequences of organic reactions that build complexity, starting with commercially available compounds and proceeding through typically six to ten chemical steps. Each step is most commonly run in a separate batch reactor - a vessel akin to a laboratory flask, but larger and more sophisticated, to enable the production of active pharmaceutical ingredients (APIs) on kilogram to tonne scales, as required. But on page 329 of this issue, Tsubogo and colleagues describe a different approach to making the anti-inflammatory drug (R)-rolipram: a fully continuous synthesis in which the raw materials flow through a sequence of solid catalysts.

机译：药物的活性成分通常是具有化学基团精确排列的结构复杂的有机分子。它们是使用有机反应的顺序制备的，这些顺序会增加复杂性，首先是从市售化合物开始，然后通常进行六到十个化学步骤。每个步骤通常在单独的间歇式反应器中进行-类似于实验室烧瓶的容器，但更大，更复杂，可以根据需要以千克至吨的规模生产活性药物成分（API）。但是在本期的第329页上，Tsubogo及其同事描述了制备抗炎药（R）-咯利普兰的另一种方法：完全连续的合成，其中原料流经一系列固体催化剂。

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《Nature》 |2015年第7547期|302-303|共2页
作者
JOEL M. HAWKINS;
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作者单位

Chemical Research and Development, Pfizer Worldwide Research and Development, Groton, Connecticut 06340, USA;

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收录信息美国《科学引文索引》(SCI);美国《工程索引》(EI);美国《生物学医学文摘》(MEDLINE);美国《化学文摘》(CA);
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正文语种 eng
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1. Streamlining amine synthesis Bulky amine groups that help make many drugs more bioavailable can be added readily to organic compounds [J] . Kuerti Laszlo Science . 2015,第6237期

机译：简化胺的合成可以很容易地将有助于使许多药物具有更高生物利用率的大容量胺基团添加到有机化合物中
2. A C-H oxidation approach for streamlining synthesis of chiral polyoxygenated motifs Dedicated to Professor Paul Wender for his pioneering and inspirational work on complexity generating organometallic reactions for streamlining complex molecule synthesis [J] . Covell D.J., White M.C. Tetrahedron . 2013,第36期

机译：一种C-H氧化方法，用于简化手性多加氧基序的合成致敬Paul Wender教授，他在复杂性生成有机金属反应以简化复杂分子合成方面的开创性和启发性工作
3. CHANGES AT THE VETERINARY DRUGS DIRECTORATE: >Streamlining the Emergency Drug Release and Drug Adverse Reaction Programs [J] . The Canadian veterinary journal . 2002,第5期

机译：兽药目录的变化：>简化紧急药物释放和药物不良反应程序
4. Streamlining Chemoproteomics Technology for Rapid Target Identification in Drug Discovery [C] . Hua Tang, Jeff Olson, Paul Richardson, American Society for Mass Spectrometry Conference on Mass Spectrometry and Allied Topics . 2010

机译：精简化学策略技术，用于毒品发现中快速目标鉴定
5. Application of Nitrene Transfer Reactions for Streamlining Amine Synthesis Part One: Development of C–H Amination via Metal-Catalyzed Nitrene Transfer Part Two: Stereocontrolled 4pi-Electrocyclization via Eneallene Aziridination [D] . Corbin, Joshua Robert. 2020

机译：硝酸硝基转移反应在精简胺合成中的应用部分：通过金属催化的硝酸丁烯转移第2部分进行C-H胺化：通过Eneallensαziridination立体控制4PI电循环
6. Streamlining staging of lung and colorectal cancer with whole body MRI; study protocols for two multicentre non-randomised single-arm prospective diagnostic accuracy studies (Streamline C and Streamline L) [O] . Stuart A. Taylor, Sue Mallett, Anne Miles, 2017

机译：全身MRI简化了肺癌和大肠癌的分期；两个多中心非随机单臂前瞻性诊断准确性研究的研究方案（流线C和流线L）
7. Streamlining drug synthesis [O] . Joel M. Hawkins 2015

机译：精简药物合成

Streamlining drug synthesis

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