Geron Corporation

Jale Muslehiddinoglu

Jennifer Elizabeth Albaneze-Walker

Dinesh Gala

The present invention relates to a process for preparing the telomerase inhibitor imetelstat using a 3 steps per cycle solid-phase support bound process comprising the steps of deprotection of the 3′-amino group of the support-bound oligonucleotide, coupling with a 5′-phosphoramidite, and sulfurization with an acyl disulfide, characterized by the absence of an additional capping step in each cycle that is used to prevent unreacted 3′-amino oligonucleotide groups from reacting during subsequent cycles. Imetelstat has formula below.

Process for preparing imetelstat

The present invention relates to a process for preparing the telomerase inhibitor imetelstat using a 3 steps per cycle phase support bound process comprising the steps of deprotection of the 3'-amino group of the support-bound oligonucleotide, coupling with a 5&#x2032;-phosphoramidite, and sulfurization with an acyl disulfide, characterized by the absence of an additional capping step in each cycle that is used to prevent unreacted 3&#x2032;-amino oligonucleotide groups from reacting during subsequent cycles. Imetelstat has formula below. 

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Beerse, Belgium

Jale Muslehiddinoglu