化学
酮
醛
试剂
产量(工程)
酒
人类免疫缺陷病毒(HIV)
组合化学
催化作用
药品
卤化物
有机化学
病毒学
药理学
医学
生物
材料科学
冶金
作者
Juan C. Caravez,Yuting Hu,Erfan Oftadeh,Kirubel T. Mamo,Bruce H. Lipshutz
标识
DOI:10.1021/acs.joc.3c02855
摘要
A very efficient four-step synthesis of the main fragment of Gilead's anti-HIV drug lenacapavir is described. The route showcases a 1,2-addition to an intermediate aldehyde using an organozinc halide derived from a commercially available difluorobenzyl Grignard reagent. This sets the stage for the oxidation of the resulting secondary alcohol to the desired ketone, which relies solely on catalytic amounts of TEMPO together with NaClO as the terminal oxidant, affording the targeted ketone in 67% overall yield.
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