Working Paper
Authors
- Bin Zheng ,
- Chao Hang ,
- Jason Zhu ,
- Geoffrey Purdum ,
- Melda Sezen-Edmonds ,
- Daniel Treitler ,
- Miao Yu ,
- Changxia Yuan ,
- Ye Zhu ,
- Adam Freitag ,
- Siwei Guo ,
- Guanghui Zhu ,
- Benjamin Hritzko ,
- James Paulson ,
- Jonanthan Shackman ,
- Brian He ,
- Weiqing Fu ,
- HuaChia Tai ,
- Sloan Ayers ,
- Hyunsoo Park ,
- Martin Eastgate ,
- Benjamin Cohen ,
- Amanda Rogers ,
- Qinggang Wang ,
- Michael A. Schmidt
Bristol Myers Squibb
Abstract
A highly stereoselective synthesis of a cyclic dinucleotide (CDN) STING
agonist containing two chiral thiophosphoramidate linkages is described. These rare, yet key functional groups were, for
the first time, installed efficiently and with high diastereoselectivity using
a specially designed P(V) reagent. By
utilizing this strategy, the CDN was prepared in greater than sixteen-fold
higher yield than the prior P(III) approach, with fewer hazardous reagents and chromatographic
purifications.
Content

Supplementary material

BMS Diastereoselective CDN Synthesis-Supporting Information