[EN] COMPOUNDS AND PROCESSES FOR THE PREPARATION OF ERIBULIN [FR] COMPOSÉS ET PROCÉDÉS POUR LA PRÉPARATION D'ÉRIBULINE
摘要:
The present invention relates to compounds and a process for the preparation of eribulin. More specifically, the process to prepare the C14- C35 sulfone fragment of eribulin (i.e. compounds of formula I) by reacting a C14-C26 ketone fragment of eribulin (i.e. compounds of formula II) with a C27-C35 sulfonium salt fragment (i.e. compounds of formula III) under Corey-Chaykovsky reaction conditions is explored. The processes to prepare the intermediate C14-C26 ketone (i.e. compounds of formula II), the intermediate C27-C35 sulfonium salt (i.e. compounds of formula III) and the intermediate C27-C35 aldehyde (i.e. compounds of formula IV) arc also disclosed.
[EN] COMPOUNDS AND PROCESSES FOR THE PREPARATION OF ERIBULIN [FR] COMPOSÉS ET PROCÉDÉS POUR LA PRÉPARATION D'ÉRIBULINE
摘要:
The present invention relates to compounds and a process for the preparation of eribulin. More specifically, the process to prepare the C14- C35 sulfone fragment of eribulin (i.e. compounds of formula I) by reacting a C14-C26 ketone fragment of eribulin (i.e. compounds of formula II) with a C27-C35 sulfonium salt fragment (i.e. compounds of formula III) under Corey-Chaykovsky reaction conditions is explored. The processes to prepare the intermediate C14-C26 ketone (i.e. compounds of formula II), the intermediate C27-C35 sulfonium salt (i.e. compounds of formula III) and the intermediate C27-C35 aldehyde (i.e. compounds of formula IV) arc also disclosed.