855300-90-2Relevant articles and documents
Preparation method of stable isotope-labeled clorprenaline
-
Paragraph 0037-0039, (2021/07/24)
The invention relates to a preparation method of stable isotope-labeled clorprenaline. The preparation method comprises the following steps: with 2-bromo-2'-chloroacetophenone as an initial raw material, successively conducting improved Gabriel synthesis (wherein the initial raw material and an amination reagent sodium, namely diformyl amide are subjected to a nucleophilic substitution reaction), hydrolysis, reduction and reductive amination so as to synthesize the isotope-labeled clorprenaline . According to the preparation method disclosed by the invention, through a four-step conventional chemical reaction, process design is reasonable, raw material price is low, an experimental process is controllable, operation is simple and convenient, various required labeled compounds such as D-labeled, 13C-labeled or D/13C double-labeled compounds can be conveniently synthesized, the purity of the prepared target product is high and reaches 98% or above, total yield reaches 66% or above, the isotope abundance of the final product can reach 98% or above, the phenomenon of isotope abundance dilution is avoided, higher reproducibility and stability are achieved, and the obtained target compound can provide a standard reagent for accurately and quantitatively detecting trace residues of clorprenaline.
