Synthesis of HIV protease inhibitors atazanavir sulfate
BAI Yue-fei
PI Chang-qiao
WU Xiao-jing
LIU Ju
ZHOU Peng
ZHOU Kai
Abstract：Objective: To study the synthetic technology of atazanavir sulfate. Methods: Tert-butyl (2 S, 3 S)-4-chloro-3-hydroxy-1-phenylbutan-2-ylcarbamate was used as the starting material and treated by SN2 reaction, intramolecular rearrangement, Boc-protection, cyclization, epoxide ring aminolysis, followed by deprotection, salifying, neutralization, condensation, and ion exchange resin reaction to get the target product. Results: The structure of atazanavir sulfate with an overall yield of 61. 2％ by starting material meter was confirmed by1 H-NMR, 13 C-NMR and MS, and the purity was 99. 8％ estimated by HPLC. Conclusion: This synthetic process is available raw materials, easy operation, high yield, and has good quality production. In conclusion, it has feasibility of industrial production.
Keywords：atazanavir sulfateHIV protease inhibitorsynthesis
Publication Date：2018-01-01
Online Publishing Date：2026-08-14(First online date of this platform, not the publication date of the document)
Pages：5( 1798-1802 )