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. 2025 Apr 2;147(13):11036-11048.
doi: 10.1021/jacs.4c15966. Epub 2025 Mar 24.

Total Synthesis of Enlicitide Decanoate

Hongming Li  1 , David A Thaisrivongs  1 , Gao Shang  1 , Yonggang Chen  1 , Qinghao Chen  1 , Lushi Tan  1 , Kai-Jiong Xiao  1 , Reed T Larson  1 , Jeffrey T Kuethe  1 , Joshua Lee  1 , Nicholas R Deprez  1 , Andrew F Nolting  1 , Marc Poirier  1 , Paul G Bulger  2 , Erik L Regalado  2 , Mirlinda Biba  2 , Fuh-Rong Tsay  2 , Jimmy DaSilva  2 , Chris K Prier  1 , Christopher A Strulson  2 , Kerstin Zawatzky  2 , Zhu Liu  2 , Justin A Newman  2 , Kathleen Sokolowsky  2 , Weijuan Tang  2 , Kari Hullen  2 , Nimisha Thakur  2 , Cody Welch  2 , Smit Patel  2 , Yu He  2 , Jing Xu  2 , Narayan Variankaval  2 , Artis Klapars  1 , Jongrock Kong  1 , Richard Desmond  1 , Richard Varsolona  2 , Peter E Maligres  1 , Carlos A Pons Siepermann  1 , Lee Robison  2 , Tiffany Piou  1 , Clara Hartmanshenn  1 , Anagha Chandra  1 , Anisha Patel  2 , Marc R Becker  1 , Guiquan Liu  3 , Jianjun Duan  3 , Baoqiang Wan  3 , Chengqian Xiao  3 , Yongpeng Yuan  3 , Xiaohui Cao  3 , Lu Chen  3 , Ruxia Yi  3 , Zheng Wu  3 , Minyi Feng  3 , Donghong Li  4 , Zhiyan Song  4 , Yawei Dong  4 , Julin Sun  4 , Biao Li  4 , Guangxin Shao  4 , Louis-Charles Campeau  1 , Jingjun Yin  1
Affiliations

Total Synthesis of Enlicitide Decanoate

Hongming Li et al. J Am Chem Soc. .

Abstract

We report the total synthesis of enlicitide decanoate, an orally bioavailable inhibitor of proprotein convertase subtilisin/kexin type 9 that is being developed for the treatment of atherosclerotic cardiovascular disease. It is a highly complex macrocyclic peptide with a significant number of nonpeptide structural elements that presents a daunting synthetic chemistry challenge. We describe the development of a convergent, efficient, and robust manufacturing process that enables the large-scale production of enlicitide.

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