Bempedoic Acid

Bempedoic Acid serves as a pivotal pharmaceutical intermediate and active pharmaceutical ingredient (API) in the industrial synthesis of lipid-lowering therapies, most notably for patients with hypercholesterolemia who are statin-intolerant or require additional LDL-C reduction beyond statin therapy. As the first-in-class ACL inhibitor, Bempedoic Acid offers a differentiated mechanism of action that complements statin therapy while avoiding the muscle-related side effects commonly associated with statins. In quality control contexts, Bempedoic Acid is supplied with detailed characterization data compliant with regulatory guidelines, making it suitable for analytical method development, method validation (AMV), and quality control (QC) applications for Abbreviated New Drug Applications (ANDA). The unique dicarboxylic acid scaffold of Bempedoic Acid also serves as a versatile building block in drug discovery programs exploring novel metabolic and anti-inflammatory agents.

 

Product Parameters

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Parameter	Specification
Product Name	Bempedoic Acid
CAS Number	738606-46-7
Molecular Formula	C₁₉H₃₆O₅
Molecular Weight	344.49 g/mol
Appearance	White to off-white solid
Melting Point	87 – 92°C
Boiling Point	506.5 ± 35.0°C (predicted)
Density	1.045 ± 0.06 g/cm³ (predicted)
pKa	4.55 ± 0.45 (predicted)
Storage Condition	Refrigerator

 

Non-statin lipid-lowering drugs

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Bempedoic Acid is a novel non-statin lipid-lowering agent used for the treatment of hypercholesterolemia. It reduces serum levels of low-density lipoprotein cholesterol (LDL-C) by upregulating low-density lipoprotein (LDL) receptors and enhancing LDL clearance.

 

Effects and Actions

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Bempedoic Acid is indicated for the treatment of adult patients with heterozygous familial hypercholesterolemia (HeFH) or confirmed atherosclerotic cardiovascular disease (ASCVD) who require further reduction of LDL-C levels but cannot achieve the target with the maximum tolerated dose of statins. In clinical trials, it has demonstrated significant efficacy in lowering LDL-C levels, along with favorable safety and tolerability profiles.

 

Syntjetic Route

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Using 317 kg of ethyl isobutyrate (147) as the starting material, an alkylation reaction was carried out with an alkyl bromide (148), followed by the Finkelstein reaction to yield alkyl iodide 149. Alkyl iodide 149 was then reacted with 0.5 equivalents of methanesulfonyl isocyanate under alkaline conditions to promote the dialkylation of iodide 149, yielding the intermediate isonitrile 150. Instead of being separated, isonitrile 150 was directly processed in Chemicalbook isopropanoic acid under acidic conditions. By adjusting the pH, ketone 151 was obtained with excellent yield based on the mass of isonitrile 150. Ketone 151 was reduced with sodium borohydride and subsequently subjected to saponification to yield a crude active pharmaceutical ingredient (API). Following a series of crystallization steps, bempedoic acid was further purified with high yield. Notably, this synthetic route has been validated at scales exceeding 300 kg.

 

Contact Us

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Need Bempedoic Acid for your lipid-lowering API manufacturing campaign, impurity profiling program, or analytical method development? Cosperpharm delivers with the quality, documentation, and supply reliability you require. Reach out to our team today — we respond within 2 business hours.