Practical Synthesis of MDM2 Antagonist RG7388. Part 2: Development of the Cu(I) Catalyzed [3 + 2] Asymmetric Cycloaddition Process for the Manufacture of Idasanutlin
A concise catalytic asymmetric synthesis of idasanutlin (1) was developed in which the key pyrrolidine core, containing four contiguous stereocenters, was constructed via a Ag/MeOBIPHEP promoted [3 + 2] cycloaddition reaction.
Unit Operation: Reaction
Objective: Design
Company: Roche
Source: Org. Process Res. Dev., 2016, 20 (12), pp 2057–2066
Authors: Andre Alker (Roche), Marcello Bosco (Roche), Ralph Diodone (Roche), Dan Fishlock (Roche), Stefan Hildbrand (Roche), Bernd Kuhn (Roche), Christian Moessner (Roche), Carsten Peters (Roche), Pankaj D. Rege (Roche), Gösta Rimmler (Roche), Markus Schantz (Roche)
Publish Date: 31-Oct-2016
Copyright © 2018 Scale-up Systems Ltd. | DynoChem Software and Development Services for the Pharma Industry | Privacy | Cookies | Contact