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Synthesis
DOI: 10.1055/a-2816-6824
Paper

Pyrrolo[2,3-h]tetrahydroisoquinoline Derivatives Exhibiting Mixed Dopaminergic D 3 >D 2 and Serotoninergic 5-HT 6 affinity

Authors

  • Ferenc Bertha

    1   Directorate of Drug Substance Development, EGIS Pharmaceuticals PLC, Budapest, Hungary (Ringgold ID: RIN58965)

  • Márta Porcs-Makkay

    1   Directorate of Drug Substance Development, EGIS Pharmaceuticals PLC, Budapest, Hungary (Ringgold ID: RIN58965)

  • Judit Halász

    1   Directorate of Drug Substance Development, EGIS Pharmaceuticals PLC, Budapest, Hungary (Ringgold ID: RIN58965)

  • Gábor Németh

    1   Directorate of Drug Substance Development, EGIS Pharmaceuticals PLC, Budapest, Hungary (Ringgold ID: RIN58965)

  • Simon Horváth

    1   Directorate of Drug Substance Development, EGIS Pharmaceuticals PLC, Budapest, Hungary (Ringgold ID: RIN58965)

  • Miklós Nyerges

    2   Early Process Development, Servier Research Institute of Medicinal Chemistry, Budapest, Hungary (Ringgold ID: RIN248305)

  • Anne Rojas

    3   Institut de Recherches Servier, Institut de Recherches Internationales Servier, Suresnes, France (Ringgold ID: RIN154729)

  • Jean-Claude Ortuno

    3   Institut de Recherches Servier, Institut de Recherches Internationales Servier, Suresnes, France (Ringgold ID: RIN154729)

  • Gyöngyvér Pusztai

    1   Directorate of Drug Substance Development, EGIS Pharmaceuticals PLC, Budapest, Hungary (Ringgold ID: RIN58965)

  • Zsófia Garádi

    1   Directorate of Drug Substance Development, EGIS Pharmaceuticals PLC, Budapest, Hungary (Ringgold ID: RIN58965)

  • Simig Gyula

    1   Directorate of Drug Substance Development, EGIS Pharmaceuticals PLC, Budapest, Hungary (Ringgold ID: RIN58965)

  • Balázs Volk 

    1   Directorate of Drug Substance Development, EGIS Pharmaceuticals PLC, Budapest, Hungary (Ringgold ID: RIN58965)
Further Information
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A series of pyrrolo[2,3-h]tetrahydroisoquinoline derivatives has been synthesized and shown to be potent ligands at the 5-HT 6 , D 2 and D 3 receptors. By systematically changing the structural elements, we have arrived atexhibiting the targeted receptor profile, considered to be potentially effective for the treatment of neurodegenerative disorders related to schizophrenia. In the course of the elaboration of the synthetic routes, several new tetrahydroisoquinoline derivatives as versatile synthetic building blocks have been prepared.



Publication History

Received: 12 January 2026

Accepted after revision: 18 February 2026

Accepted Manuscript online:
18 February 2026

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