雷尼镍业
产量(工程)
立体选择性
高效液相色谱法
谷氨酰胺
化学
组合化学
有机化学
催化作用
材料科学
氨基酸
生物化学
冶金
作者
Hongjian Qin,Jin Chen,Abdullajon Odilov,Emmanuel Mintah Bonku,Fuqiang Zhu,Qi Liu,Jingshan Shen,Haji Akber Aisa
标识
DOI:10.1021/acs.oprd.2c00225
摘要
In this study, the development of a concise alternative process for synthesis of a key nirmatrelvir intermediate cyclic glutamine analog is described. The process proceedes via α-cyanomethylation of dimethyl N-BocGlu in the presence of NdCl3, followed by one-pot Raney nickel-catalyzed hydrogenation of the cyano group with concomitant cyclization and ammonolysis and subsequent deprotection of N-Boc to deliver the target intermediate cyclic glutamine analog in three steps with an 82% overall yield and 99.4 A% high-performance liquid chromatography (HPLC) purity. This study resulted in improved synthetic efficiency and stereoselectivity of α-cyanomethylation for production of a key nirmatrelvir intermediate cyclic glutamine analog.
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