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从可的松到恩利昔肽:默克公司的合成化学创新之旅。

From Cortisone to Enlicitide: A Journey of Synthetic Chemistry Innovations at Merck.

作者信息

Campeau Louis-Charles

机构信息

Process Research and Development, Merck & Co., Inc., 126 East Lincoln Avenue, Rahway, New Jersey 07065, United States.

出版信息

J Org Chem. 2025 Apr 11;90(14):4781-4795. doi: 10.1021/acs.joc.4c02919. Epub 2025 Apr 1.

Abstract

Necessity is the mother of invention. Most synthetic chemistry innovations are driven by our desire to make molecules. In the first half of the 20th century, much of this work was inspired by natural products, but as we started to understand the impact that specific molecules could have on biology and human health, a new stimulus for invention appeared. The pharmaceutical industry first brought mass production and formulation of natural products for medicinal purposes but quickly started tinkering with molecular structure to modify compounds' properties, eventually designing molecules from scratch. This necessity for invention of new molecules to improve human health and to manufacture them on large scale is an excellent stimulus for synthetic chemistry innovations. In this Perspective, examples from Merck's chemistry groups are used to highlight the types of innovations that can arise from these endeavors.

摘要

需要乃发明之母。大多数合成化学创新是由我们制造分子的欲望驱动的。在20世纪上半叶,这项工作大多受到天然产物的启发,但随着我们开始理解特定分子对生物学和人类健康可能产生的影响,一种新的发明刺激因素出现了。制药行业首先将天然产物进行大规模生产和配制用于医疗目的,但很快就开始对分子结构进行调整以改变化合物的性质,最终开始从头设计分子。这种为改善人类健康而发明新分子并进行大规模生产的需求,是合成化学创新的绝佳刺激因素。在这篇视角文章中,默克化学团队的例子被用来突出这些努力可能产生的创新类型。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/45b3/11998012/804d3ad2c444/jo4c02919_0004.jpg

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