258516-82-4Relevant articles and documents
Synthesis method and application of propofol sodium and intermediate thereof
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Paragraph 0025; 0026; 0029-0036, (2021/09/22)
The method comprises an intermediate B and an intermediate C, and, the application of the phosphorus propofol sodium prepared by the synthesis method in an animal anesthetic sedative. The phosphorus propofol sodium synthesis method provided by the invention avoids the use of highly toxic reagent chlorobromomethane and is high in safety. The prepared propofol intermediate reaction condition is mild, the operation is simple and convenient, the quality yield is > 97%, and the propofol prodrug synthesized by the synthetic method provided by the invention can generate the same clinical effect as the commercially available propofol emulsion injection.
Monodisperse oligoethylene glycols modified Propofol prodrugs
Deng, Tao,Mao, Xianglan,Li, Yu,Bo, Shaowei,Yang, Zhigang,Jiang, Zhong-Xing
supporting information, p. 3502 - 3505 (2018/10/15)
The low water solubility of Propofol resulted in complicated formulation and adverse effects during its clinical application. To improve its water solubility and maintain its anesthetic effects, Propofol prodrugs with monodisperse oligoethylene glycols as solubility enhancer were designed and synthesized. Monodisperse oligoethylene glycols enable the concise manipulation of water solubility, biocompatibility and anesthetic effects. Through the physicochemical and biological assay, a few water soluble prodrugs of Propofol were identified as promising anesthetic to overcome the drawbacks associated with Propofol.
Synthesis, in vitro and in vivo characterization of novel ethyl dioxy phosphate prodrug of propofol
Kumpulainen, Hanna,Jaervinen, Tomi,Mannila, Anne,Leppaenen, Jukka,Nevalainen, Tapio,Maentylae, Antti,Vepsaelaeinen, Jouko,Rautio, Jarkko
, p. 110 - 117 (2008/09/19)
A novel ethyl dioxy phosphate prodrug of propofol (3) was synthesized and characterized in vitro and in vivo as safer alternative for phosphonooxymethyl prodrugs. The synthesis of 3 was achieved via vinyl and 1-chloroethyl ether intermediates, followed by