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- W4313448466 abstract "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." @default.
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- W4313448466 date "2022-12-20" @default.
- W4313448466 modified "2023-09-27" @default.
- W4313448466 title "Optimized Synthesis of a Key Intermediate of Nirmatrelvir" @default.
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- W4313448466 doi "https://doi.org/10.1021/acs.oprd.2c00225" @default.
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