JOURNAL ARTICLE

Synthesis of Carbon 14 and Deuterium‐Labelled Nerandomilast (BI 1015550).

  • Published In: Journal of Labelled Compounds & Radiopharmaceuticals, 2025, v. 68, n. 1/2. P. 1 1 of 3

  • Database: Academic Search Ultimate 2 of 3

  • Authored By: Latli, Bachir; Hrapchak, Matt J.; Frutos, Rogelio P. 3 of 3

Abstract

(R)‐2‐(4‐(5‐Chloropyrimidin‐2‐yl)piperidin‐1‐yl)‐4‐((1‐(hydroxymethyl)cyclobutyl)amino)‐6,7‐dihydrothieno[3,2‐d]pyrimidine 5‐oxide (BI 1015550, 1) is a potent and selective inhibitor of phosphodiesterase type 4 (PDE4) being developed for the treatment of idiopathic pulmonary fibrosis (IPF) and progressive pulmonary fibrosis (PPF). We report the synthesis of this drug candidate labelled with carbon 14 and deuterium. The carbon 14 synthesis was completed in three radioactive steps in 27% overall yield, with a specific activity of 52 mCi/mmol (1.92 GBq/mmol), radiochemical purity, and enantiomeric excess higher than 99%. The deuterium labelled compound was prepared in seven steps in 67% overall yield and with isotopic enrichment, chemical purity, and enantiomeric excess higher than 99%. [ABSTRACT FROM AUTHOR]

Additional Information

  • Source:Journal of Labelled Compounds & Radiopharmaceuticals. 2025/01, Vol. 68, Issue 1/2, p1
  • Document Type:Article
  • Subject Area:Chemistry
  • Publication Date:2025
  • ISSN:0362-4803
  • DOI:10.1002/jlcr.4133
  • Accession Number:184016619
  • Copyright Statement:Copyright of Journal of Labelled Compounds & Radiopharmaceuticals is the property of Wiley-Blackwell and its content may not be copied or emailed to multiple sites without the copyright holder's express written permission. Additionally, content may not be used with any artificial intelligence tools or machine learning technologies. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)

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