Optimization of the Green Synthesis Process of Sufentanil Citrate
Objective To optimize the green synthesis process of sufentanil citrate.Methods With N-Boc-piperidone,aniline,and 2-(2-thiophene)ethanol as active pharmaceutical ingredients(API),sufentanil was obtained through Bargellini,esterification,reduction,methylation,deprotection,sulfonation,N-alkylation,and acylation reactions.Finally,sufentanil citrate was obtained by salt formation.Results The optimal green synthesis process avoided the use of highly toxic reagents cyanides and palladium on carbon hydrogenation debenzylation processes,and the purity of the final product could reach over 99.5％.Conclusion The optimal synthesis process of sufentanil citrate has the advantages of cheap and easily obtainable API,mild reaction conditions,simple operation,and high process safety,which can ensure the quality and safety of the drug and is suitable for green industrial-scale production.
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