兴奋剂
药理学
基因
化学
干扰素基因刺激剂
医学
受体
生物化学
先天免疫系统
作者
Thomas W. Lyons,David A. Thaisrivongs,Nadine Kuhl,Cheol K. Chung,Angie R. Angeles,Dietrich Steinhuebel,Erik D. Guetschow,Andrew P. J. Brunskill,Timothy J. Henderson,Brandon Cash,Andrew M. Haidle
标识
DOI:10.1021/acs.oprd.4c00102
摘要
The first GMP synthesis of MK-2118, a small molecule agonist of the stimulator of interferon genes (STING) is described. The small molecule represents a dramatic change in the chemical matter from the more complex cyclic dinucleotides previously disclosed. In this article, we detail the route-scouting, decision-making, and development details of a first GMP campaign typical for a first delivery on an accelerated timeline. The route chosen involves a key copper-mediated Negishi coupling using a chiral organozinc reagent and subsequent direct isolation. Several unexpected challenges are outlined, which highlight the difficulty in developing a first scale-up process.
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