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Synthesis
DOI: 10.1055/a-2779-3222
DOI: 10.1055/a-2779-3222
Short Review
Published as part of the Special Issue dedicated to Dr. Dani Schultz, recipient of
the 2025 Dr. Margaret Faul Women in Chemistry Award
Recent Progress in Catalytic Asymmetric Pictet–Spengler Reaction to Construct 1,1-Disubstituted Scaffolds
Authors
Supported by: National Institute of General Medical Sciences R35 GM128895
Abstract
1,1-Disubstituted tetrahydroisoquinolines (THIQs) and tetrahydro-ß-carbolines (THBCs) are key intermediates in the synthesis of various alkaloid natural products. These 1,1-disubstituted scaffolds are typically constructed via the Pictet–Spengler reaction. The asymmetric catalytic variant of this reaction enables access to stereochemically pure compounds with significant biological properties. This review focuses on recent progress in organocatalyzed and enzyme-catalyzed asymmetric Pictet–Spengler reactions to generate these 1,1-disubstituted motifs.
Publication History
Received: 14 November 2025
Accepted after revision: 26 December 2025
Accepted Manuscript online:
29 December 2025
Article published online:
23 January 2026
© 2026. Thieme. All rights reserved.
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