1151665-78-9Relevant academic research and scientific papers
Method for preparing antiviral drug oseltamivir phosphate intermediate tert-butylamine derivative I
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Paragraph 0035, (2020/06/05)
The invention discloses a method for preparing a tert-butylamine derivative, and relates to the field of drug synthesis. The method comprises the following steps: 1, preparing a magnesium-amine compound, namely, adding magnesium halide and tert-butylamine A into an aprotic solvent, and carrying out a mixing stirring reaction for 0.5-1.5 h at a temperature of 0-15 DEG C to prepare a mixed solutionA; 2, adding a compound B into the mixed solution A prepared in the step 1, and carrying out a stirring reaction for more than 8 hours to prepare a mixed solution B; and 3, supplementing tert-butylamine D into the mixed solution B prepared in the step 2, and carrying out a stirring reaction for 24-48h at a temperature of 50-70 DEG C to prepare a tert-butylamine derivative I. By controlling the preparation temperature of the compound, the addition mode of tert-butylamine and the time of the ring-opening reaction, the curing phenomenon in the reaction and the increase of by-products can be effectively controlled.
A short and practical synthesis of oseltamivir phosphate (tamiflu) from (-)-shikimic acid
Nie, Liang-Deng,Shi, Xiao-Xin,Kwang, Hyok Ko,Lu, Wei-Dong
experimental part, p. 3970 - 3973 (2009/10/01)
(Chemical Equation Presented) Oseltamivir phosphate (1) was synthesized from (-)-shikimic acid through a short and practical synthetic route via eight steps in 47% overall yield. In addition, the highly regioselective and stereoselective nucleophilic replacement of OMs by the N3 group in the third and seventh steps has been studied in detail, and the reaction conditions were optimized.
