Synthesis 2019; 51(04): 971-975
DOI: 10.1055/s-0037-1610316
paper
© Georg Thieme Verlag Stuttgart · New York

Late-Stage Sulfoximination: Improved Synthesis of the Anticancer Drug Candidate Atuveciclib

Thomas Glachet
a   Normandie Université, ENSICAEN, UNICAEN, CNRS, LCMT, 14000 Caen, France   Email: vincent.reboul@ensicaen.fr
,
Xavier Franck
b   Normandie Université, CNRS, UNIROUEN, INSA Rouen, COBRA, 76000 Rouen, France
,
a   Normandie Université, ENSICAEN, UNICAEN, CNRS, LCMT, 14000 Caen, France   Email: vincent.reboul@ensicaen.fr
› Author Affiliations
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