Total Synthesis of Chrysosporazines B and C

Organic Letters 2026

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Authors: Xiaoyu Fang, Yu Jiang, Yuhan Xiao, Chenqi Wang, Ai-Jun Ma, Junyang Liu, Jia‐Lei Yan
DOI: 10.1021/acs.orglett.6c00038
Cited by: 3
References: 32

Abstract

The first total synthesis of chrysosporazines B and C was accomplished in a concise and highly stereoselective manner with overall yields of 9.2% and 8.0%, respectively. Highlights of the synthesis include a Suzuki–Miyaura coupling of E -enol tosylate followed by Rh-catalyzed asymmetric hydrogenation to establish the nonsymmetric β,β-diaryl amino acid motif, a piperazinedione condensation and reduction to construct the piperazine framework, and a late-stage Pd-catalyzed carbonylation to furnish the hexahydro-6 H -pyrazino[1,2- b ]isoquinolin-6-one scaffold.

Fields of Study & Subjects

Synthetic Organic Chemistry Methods Catalytic Cross-Coupling Reactions Cyclopropane Reaction Mechanisms

Publication details

Journal / source
Organic Letters
Publisher
American Chemical Society (ACS)
Volume
28
Issue
6
Pages
2178–2182
Publication date
2 February 2026
Language
EN