Fueling the Pipeline via Innovations in Organic Synthesis,ACS Medicinal Chemistry Letters

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Fueling the Pipeline via Innovations in Organic Synthesis
ACS Medicinal Chemistry Letters ( IF 3.5 ) Pub Date : 2021-08-27 , DOI: 10.1021/acsmedchemlett.1c00351
Eric A Voight ₁ , Stephen N Greszler ₁ , Philip R Kym ₁

Affiliation

The paramount importance of synthetic organic chemistry in the pharmaceutical industry arises from the necessity to physically prepare all designed molecules to obtain key data to feed the design–synthesis–data cycle, with the medicinal chemist at the center of this cycle. Synthesis specialists accelerate the cycle of medicinal chemistry innovation by rapidly identifying and executing impactful synthetic methods and strategies to accomplish project goals, addressing the synthetic accessibility bottleneck that often plagues discovery efforts. At AbbVie, Discovery Synthesis Groups (DSGs) such as Centralized Organic Synthesis (COS) have been deployed as embedded members of medicinal chemistry teams, filling the gap between discovery and process chemistry. COS chemists provide synthetic tools, scaffolds, and lead compounds to fuel the pipeline. Examples of project contributions from neuroscience, cystic fibrosis, and virology illustrate the impact of the DSG approach. In the first ten years of innovative science in pursuit of excellence in synthesis, several advanced drug candidates, including ABBV-2222 (galicaftor) for cystic fibrosis and foslevodopa/foscarbidopa for Parkinson’s disease, have emerged with key contributions from COS.

中文翻译：

通过有机合成创新为管道加油

合成有机化学在制药工业中的重要性源于必须对所有设计的分子进行物理准备，以获得关键数据，以支持设计-合成-数据循环，药物化学家处于该循环的中心。合成专家通过快速识别和执行有影响力的合成方法和策略来完成项目目标，解决经常困扰发现工作的合成可及性瓶颈，从而加速药物化学创新的周期。在 AbbVie，集中有机合成 (COS) 等发现合成小组 (DSG) 已被部署为药物化学团队的嵌入式成员，填补了发现和过程化学之间的空白。COS 化学家提供合成工具、支架和铅化合物来为管道提供燃料。来自神经科学、囊性纤维化和病毒学的项目贡献示例说明了 DSG 方法的影响。在追求卓越合成的前十年创新科学中，一些先进的候选药物，包括用于囊性纤维化的 ABBV-2222 (galicaftor) 和用于帕金森病的 foslevodopa/foscarbidopa，已经出现了 COS 的关键贡献。

更新日期：2021-09-09

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