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Issue 8, 2019
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Exploration of [2 + 2 + 2] cyclotrimerisation methodology to prepare tetrahydroisoquinoline-based compounds with potential aldo–keto reductase 1C3 target affinity

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Abstract

Tetrahydroisoquinoline (THIQ) is a key structural component in many biologically active molecules including natural products and synthetic pharmaceuticals. Here, we report on the use of transition-metal mediated [2 + 2 + 2] cyclotrimerisation of alkynes to generate tricyclic THIQs with potential to selectively inhibit AKR1C3.

Graphical abstract: Exploration of [2 + 2 + 2] cyclotrimerisation methodology to prepare tetrahydroisoquinoline-based compounds with potential aldo–keto reductase 1C3 target affinity

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Supplementary files

Article information


Submitted
02 Apr 2019
Accepted
27 Jun 2019
First published
27 Jun 2019

Med. Chem. Commun., 2019,10, 1476-1480
Article type
Research Article

Exploration of [2 + 2 + 2] cyclotrimerisation methodology to prepare tetrahydroisoquinoline-based compounds with potential aldo–keto reductase 1C3 target affinity

A. R. N. Santos, H. M. Sheldrake, A. I. M. Ibrahim, C. C. Danta, D. Bonanni, M. Daga, S. Oliaro-Bosso, D. Boschi, M. L. Lolli and K. Pors, Med. Chem. Commun., 2019, 10, 1476
DOI: 10.1039/C9MD00201D

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