Abstract
The synergy of a solution-phase preparation of scaffolds with a solid-phase combinatorial synthesis let to develop an efficient route to a small library of chiral, highly functionalized tetrahydroisoquinolines. Both loading on the Merrifield resin and the key acid-catalyzed Pictet-Spengler condensation were efficiently promoted by microwave irradiation. The library was designed such that up to five points of diversity would be potentially introduced, making the strategy in principle suitable for generation of a large number of compounds.
Keywords: Combinatorial chemistry, solid phase synthesis, microwave, tetrahydroisoquinoline
Combinatorial Chemistry & High Throughput Screening
Title: Microwave-Assisted, Solid-Phase Synthesis of a Chiral 1,2,3,4-Tetrahydroquinoline Library
Volume: 9 Issue: 9
Author(s): Giordano Lesma, Bruno Danieli, Francesco Lodroni, Daniele Passarella, Alessandro Sacchetti and Alessandra Silvani
Affiliation:
Keywords: Combinatorial chemistry, solid phase synthesis, microwave, tetrahydroisoquinoline
Abstract: The synergy of a solution-phase preparation of scaffolds with a solid-phase combinatorial synthesis let to develop an efficient route to a small library of chiral, highly functionalized tetrahydroisoquinolines. Both loading on the Merrifield resin and the key acid-catalyzed Pictet-Spengler condensation were efficiently promoted by microwave irradiation. The library was designed such that up to five points of diversity would be potentially introduced, making the strategy in principle suitable for generation of a large number of compounds.
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Cite this article as:
Lesma Giordano, Danieli Bruno, Lodroni Francesco, Passarella Daniele, Sacchetti Alessandro and Silvani Alessandra, Microwave-Assisted, Solid-Phase Synthesis of a Chiral 1,2,3,4-Tetrahydroquinoline Library, Combinatorial Chemistry & High Throughput Screening 2006; 9 (9) . https://dx.doi.org/10.2174/138620706778700134
DOI https://dx.doi.org/10.2174/138620706778700134 |
Print ISSN 1386-2073 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5402 |
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