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

Thomas Glachet (1) , Xavier Franck (2) , Vincent Reboul (1)

1 LCMT - Laboratoire de chimie moléculaire et thioorganique
2 COBRA - Chimie Organique et Bioorganique : Réactivité et Analyse

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.

Domaines: Chimie organique; Chimie thérapeutique

Thomas Glachet, Xavier Franck, Vincent Reboul. Late-Stage Sulfoximination: Improved Synthesis of the Anticancer Drug Candidate Atuveciclib. Synthesis: Journal of Synthetic Organic Chemistry, 2019, 51 (4), pp.971-975. ⟨10.1055/s-0037-1610316⟩. ⟨hal-01926262⟩