4.5 Article

Synthesis of Bempedoic Acid through Electrochemical Decarboxylation of Dialkylated Malonic Acid

Journal

SYNTHESIS-STUTTGART
Volume 53, Issue 19, Pages 3608-3612

Publisher

GEORG THIEME VERLAG KG
DOI: 10.1055/a-1482-9822

Keywords

bempedoic acid; electrochemical synthesis; decarboxylation; malonic acid; high efficiency

Funding

  1. National Natural Science Foundation of China [21702105]

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A new six-step synthesis method with 42% overall yield for bempedoic acid is reported in this paper, with ketone formation by electrochemical decarboxylation of dialkylated malonic acid introduced as the key step. This method uses mild conditions and its high efficiency makes it potentially suitable for industrial production.
Bempedoic acid is a small-molecule inhibitor of adenosine triphosphate-citrate lyase (ACL) that is effective in the treatment of hypercholesterolemia and hypertension. In this paper, a new, six-step synthesis of bempedoic acid with 42% overall yield is reported. Ketone formation by electrochemical decarboxylation of dialkylated malonic acid is introduced as the key step of this process. This method uses mild conditions and its high efficiency makes it potentially suitable for industrial production.

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