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1. (WO2018100050) PROCESS FOR THE PREPARATION OF AN INTERMEDIATE FOR THE SYNTHESIS OF CARFILZOMIB

Pub. No.:    WO/2018/100050    International Application No.:    PCT/EP2017/080950
Publication Date: Fri Jun 08 01:59:59 CEST 2018 International Filing Date: Fri Dec 01 00:59:59 CET 2017
IPC: C07D 303/12
Applicants: ENANTIA, S.L.
Inventors: PASTÓ AGUILÀ, Mireia
ÉCIJA QUERALT, Marta
Title: PROCESS FOR THE PREPARATION OF AN INTERMEDIATE FOR THE SYNTHESIS OF CARFILZOMIB
Abstract:
The present invention provides a compound which is the trichloroacetic acid salt of a compound of Formula (II) wherein R is selected from the group consisting of H, CH3-, (CH3)2CH-, (CH3)2CHCH2-, CH3CH2CH(CH3)-, and PhCH2-, and a process for its preparation. Formula (II) Also provided is a process for its preparation based on the stereoselective epoxidation of the corresponding olefin precursor and a process for the preparation of several pharmaceutically active ingredients comprising the preparation of the compound of formula (II).