316173-28-1Relevant articles and documents
Method for preparing peramivir intermediate
-
Paragraph 0028; 0029; 0033; 0037; 0041; 0045; 0046; 0047, (2017/04/03)
The invention discloses a method for preparing a peramivir intermediate. The method comprises the steps that 1, in the presence of a compound shown as the formula C and triethylamine, (1S,4R)-(-)-methyl-[[(1,1-dimethyl oxethyl)carbonyl]amidogen]cyclopentene-2-alkene-1-methyl heptine carbonate and 2-ethyl-N-hydroxyl imide chloride are subjected to a contact reaction in THF, after the reaction is finished, a sodium hydroxide water solution is added into reaction liquid, reacting is carried out for 2-3 hours, the pH is adjusted to range from 5 to 7, extraction and concentration are carried out, washing is carried out with cold ethyl alcohol, and (3aR,4R,6S,6aS)-4-[[(1,1-dimethyl oxethyl)carbonyl]amidogen]-3-(1'-ethyl propyl)-3a,5,6,6a-tetralin-4H-cyclopentane[d]-isoxazole-6-carboxylic acid is obtained; 2, the product obtained in the step 1 is dissolved in dichloromethane, then tert-butylamine is added, stirring and reacting are carried out for 2 hours at the temperature of 5 DEG C to 15 DEG C, concentration is carried out, washing is carried out with cold ethyl alcohol, and drying is carried out to obtain the peramivir intermediate. The method for preparing the peramivir intermediate is high in yield, and the reaction time is greatly shortened.