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Peer-reviewedCC BY 4.0Archiv Der Pharmazie

Clarifying Problems in the Synthetic Pathway Towards Methylene‐Type Levodopa Acylals as Potential Prodrugs

  • Tobias Keydel1
  • Yann Theele2
  • Andreas Link3
  1. 1University Medical Center Rostock Rostock Germany
  2. 2Pharma Center Bonn, Pharmaceutical Institute, Pharmaceutical & Medicinal Chemistry University of Bonn Bonn Germany
  3. 3Department of Pharmaceutical/Medicinal Chemistry Institute of Pharmacy, University of Greifswald Greifswald Germany
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Abstract

Here, we report a practical synthetic pathway towards levodopa (l‐DOPA) acylals with a special emphasis on problems occurring during preparation, low yields or unmanageable side reactions, and how to circumvent them. The key step can be performed rapidly by microwave irradiation in a green chemistry manner. Final compounds can be achieved after deprotection approaches but exhibit inadequate properties in terms of stability, thwarting the adaptation of the double ester concept discussed here to the important active pharmaceutical ingredient levodopa. However, a future outlook is provided, discussing potential structural and chemical changes for stable levodopa acylals.

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Cite

BibTeXRIS
BibTeX
@article{keydel2026clarifying,
  title = {{Clarifying Problems in the Synthetic Pathway Towards Methylene‐Type Levodopa Acylals as Potential Prodrugs}},
  author = {Tobias Keydel and Yann Theele and Andreas Link},
  journal = {Archiv Der Pharmazie},
  year = {2026},
  month = oct,
  doi = {10.1002/ardp.70376},
  url = {https://doi.org/10.1002/ardp.70376},
  note = {CC BY 4.0},
}
RIS
TY  - JOUR
TI  - Clarifying Problems in the Synthetic Pathway Towards Methylene‐Type Levodopa Acylals as Potential Prodrugs
AU  - Tobias Keydel
AU  - Yann Theele
AU  - Andreas Link
PY  - 2026
DA  - 2026/10/01
JO  - Archiv Der Pharmazie
DO  - 10.1002/ardp.70376
UR  - https://doi.org/10.1002/ardp.70376
AB  - Here, we report a practical synthetic pathway towards levodopa (l‐DOPA) acylals with a special emphasis on problems occurring during preparation, low yields or unmanageable side reactions, and how to circumvent them. The key step can be performed rapidly by microwave irradiation in a green chemistry manner. Final compounds can be achieved after deprotection approaches but exhibit inadequate properties in terms of stability, thwarting the adaptation of the double ester concept discussed here to the important active pharmaceutical ingredient levodopa. However, a future outlook is provided, discussing potential structural and chemical changes for stable levodopa acylals.
SN  - 0365-6233
SN  - 1521-4184
ER  -