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Synthesis 2019; 51(04): 971-975
DOI: 10.1055/s-0037-1610316
DOI: 10.1055/s-0037-1610316
paper
Late-Stage Sulfoximination: Improved Synthesis of the Anticancer Drug Candidate Atuveciclib
This research was supported by Conseil Régional de Normandie, CNRS, Normandie Université, LabexSynorg (ANR-11-LABX-0029), and European FEDER funding.Further Information
Publication History
Received: 27 August 2018
Accepted after revision: 13 October 2018
Publication Date:
05 November 2018 (online)
Abstract
An efficient synthesis of racemic atuveciclib was accomplished in five steps with an excellent 51% overall yield, using cheap reagents and mild reaction conditions. The key sulfoximination reaction was realized during the last step of the synthesis from the corresponding sulfide.
Supporting Information
- Supporting information for this article is available online at https://doi.org/10.1055/s-0037-1610316.
- Supporting Information
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Selected examples:
Selected examples:
Selected examples:
Simultaneously, three groups worked on this synthesis, including ours:
Sulfoximines are good ligands for transition metals: