Divergent Total Synthesis of Denudatine Alkaloids Cochlearenine, Macrocentrine, Dictizine, 15‐Veratroyl‐17‐Acetyl‐19‐Oxodictizine, and the Proposed Structure of Acochlearine

Abstract The first asymmetric total syntheses of four denudatine alkaloids, cochlearenine, macrocentrine, dictizine, and 15‐veratroyl‐17‐acetyl‐19‐oxodictizine, along with the asymmetric synthesis of the proposed structure of acochlearine, were accomplished in a divergent manner. Highly fused tetracyclic skeletons (A/B/E/F rings) with different N ‐alkyl groups (Me and Et) were constructed by Brønsted acid promoted intramolecular Mannich reactions. The bicyclo[2.2.2]octane C/D rings were constructed via two‐fold intermolecular Diels–Alder reactions. By utilizing these key processes, the common intermediates, possessing the complex cage‐like hexacyclic skeleton, were constructed. From these common intermediates, the four denudatine alkaloids were synthesized through late‐stage, chemo‐ and stereoselective modifications around the A/C rings. The spectroscopic data of the proposed structure of acochlearine were inconsistent with those of natural acochlearine.

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Publication Details

Journal
Angewandte Chemie
Published
2025-12-04
DOI
https://doi.org/10.1002/ange.202521481
Primary Topic
Berberine and alkaloids research
Type
article
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article

Divergent Total Synthesis of Denudatine Alkaloids Cochlearenine, Macrocentrine, Dictizine, 15‐Veratroyl‐17‐Acetyl‐19‐Oxodictizine, and the Proposed Structure of Acochlearine

Naoya Miyamoto, Kosuke Fujioka, Hiroki Toya, Hidetoshi Tokuyama et al.
Angewandte Chemie
Berberine and alkaloids research
article

Divergent Total Synthesis of Denudatine Alkaloids Cochlearenine, Macrocentrine, Dictizine, 15‐Veratroyl‐17‐Acetyl‐19‐Oxodictizine, and the Proposed Structure of Acochlearine

Naoya Miyamoto, Kosuke Fujioka, Hiroki Toya, Hidetoshi Tokuyama, Juri Sakata, Sayaka Kawano
article en

Abstract

Abstract The first asymmetric total syntheses of four denudatine alkaloids, cochlearenine, macrocentrine, dictizine, and 15‐veratroyl‐17‐acetyl‐19‐oxodictizine, along with the asymmetric synthesis of the proposed structure of acochlearine, were accomplished in a divergent manner. Highly fused tetracyclic skeletons (A/B/E/F rings) with different N ‐alkyl groups (Me and Et) were constructed by Brønsted acid promoted intramolecular Mannich reactions. The bicyclo[2.2.2]octane C/D rings were constructed via two‐fold intermolecular Diels–Alder reactions. By utilizing these key processes, the common intermediates, possessing the complex cage‐like hexacyclic skeleton, were constructed. From these common intermediates, the four denudatine alkaloids were synthesized through late‐stage, chemo‐ and stereoselective modifications around the A/C rings. The spectroscopic data of the proposed structure of acochlearine were inconsistent with those of natural acochlearine.

Angewandte ChemieVol. 138(4)
Tohoku University (JP)
Openalex Percentile: Top 59%
Berberine and alkaloids research
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