Synthesis of Deuterium Labeled D5-JPH203 and D3-N-Acetyl JPH203

Michael F Wempe
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Michael F Wempe: Skaggs School of Pharmacy and Pharmaceutical Science, University of Colorado Anschutz Campus, Aurora, Colorado 80045, USA

Biomedical Journal of Scientific & Technical Research, 2023, vol. 49, issue 4, 40805-40812

Abstract: JPH203 is a selective LAT1 inhibitor designed to significantly reduce essential uptake and induce apoptosis by the mitochondria-dependent intrinsic apoptotic signalling pathway. A phase II active metabolite of JPH203 is N-acetyl JPH203. Herein, we report the synthesis and characterization of deuterium labelled d5 -JPH203 and d3 -N-acetyl JPH203. JPH203 is currently in Phase II clinical trials. These compounds have been successfully used as internal standards for liquid chromatography mass spectrometry-mass spectrometry (LC/MS-MS) from biological samples. Comprising fifteen steps, the synthesis of d5-JPH203 utilizes d5 -benzoyl chloride. Whereas d3 -acetyl JPH203 uses d3-acetylchloride and prepared in eighteen synthetic steps.

Keywords: Journals on Medical Drug and Therapeutics; Journals on Emergency Medicine; Physical Medicine and Rehabilitation; Journals on Infectious Diseases Addiction Science and Clinical Pathology; Open Access Clinical and Medical Journal; Journals on Biomedical Science; List of Open Access Medical Journal; Journals on Biomedical Engineering; Open Access Medical Journal; Biomedical Science Articles; Journal of Scientific and Technical Research (search for similar items in EconPapers)
Date: 2023
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Persistent link: https://EconPapers.repec.org/RePEc:abf:journl:v:49:y:2023:i:4:p:40805-40812

DOI: 10.26717/BJSTR.2023.49.007822

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