171337-01-2Relevant academic research and scientific papers
Preparation method of selegiline
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Paragraph 0072; 0074; 0078, (2019/08/14)
The invention provides a preparation method of selegiline. The method comprises the steps of carrying out an acyl chlorination reaction on a compound (i), carrying out an acylation reaction on the compound (i) and benzene, and carrying out a propargylation reaction after carbonyl reduction and deacylation to obtain selegiline, wherein in the compound (i), R represents methyl or ethyl or trifluoromethyl or phenyl or benzyl. According to the method, an acyl-D-N-methylalanine compound is used as a raw material and subjected to acylation, carbonyl reduction, the deacylation reaction and the propargylation reaction to obtain the selegiline, not only is the raw material simple and easy to obtain, but also there are few reaction steps, the operation is simple and convenient, and dangerous or high-price reagent raw materials do not need to be used. Meanwhile, according to the method, chiral resolution of an intermediate or a final product is not needed, the ee value of the product is high, theyield is high, and the method is suitable for large-scale and industrial production.
Diastereoselective Preparation of Chiral Lithiated Allyl Amines: Application in EPC-Synthesis
Yus, Miguel,Foubelo, Francisco,Falvello, Larry R.
, p. 2081 - 2092 (2007/10/03)
Lithiation of chiral allylamine (R)-1 with BunLi and ButLi leads to the formation of intermediate (R)-2, which by reaction with D2O, Me2CO or (CH2)5CO affords the expected chiral compounds (R)-3, (R)-4 and (R)-5, respectively.With Bu
