Acetaminophen Prodrug: Microwave-Assisted Synthesis and in vitro Metabolism Evaluation by Mass Spectrometry

Journal of the Brazilian Chemical Society

Clososki, Giuliano C.¹  Universidade de São Paulo, Ribeirão Preto, Brazil¹  Marques, Lucas M. M.¹  Oliveira, Anderson R. M.¹  Souza, Glória E. P.¹  Lopes, Norberto P.¹  Murie, Valter E.¹ 

关键词:  microwave;    drug synthesis;    prodrug;    propacetamol;    acetaminophen;    mass spectrometry;   

DOI  :  10.5935/0103-5053.20160005

学科分类：化学（综合）

来源: SciELO

【 摘 要 】

Propacetamol is an acetaminophen prodrug of intravenous administration used to control fever and pain of perioperative period in multimodal analgesia therapy. After injection, it is completely converted by plasma esterases into N,N-diethylglycine and acetaminophen, its active metabolite whose mechanism of action is the inhibition of prostaglandin synthesis. Herein, we report an improved protocol for the synthesis of propacetamol hydrochloride that allows the isolation of the active pharmaceutical ingredient (API) with high purity and yield. In addition, the in vitro metabolism of propacetamol in a microssomal reaction was evaluated by ion trap tandem mass spectrometry.

【 授权许可】

Unknown