6589-55-5Relevant articles and documents
Method for synthesizing chiral alpha-amino alcohol compound
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Paragraph 0083-0091, (2021/07/28)
The invention discloses a method for synthesizing a chiral alpha-amino alcohol compound. The method comprises the following steps: sequentially adding an iron catalyst, a ligand, ketone, an organic solvent and silane into a reaction system at 20-30 DEG C in a nitrogen atmosphere, then stirring the obtained mixture, and carrying out column chromatography separation on the obtained product to obtain a product, namely chiral alpha-amino alcohol. According to the invention, the most high-yield iron catalyst in earth crust is used, and cheap silane (PMHS, 500 g/298 yuan) is adopted as a reducing agent, so the asymmetric reduction reaction of alpha-amino ketone can be efficiently achieved under mild conditions so as to obtain the high-yield optically-active chiral alpha-amino alcohol compound; and moreover, through the creative labor of the inventor, reaction yield can reach 99%, and meanwhile, the content of the target product in the generated reaction product is 99%.
5-Aryloxazolidines as Reagents for Double Alkylation of Arenes: A Novel Synthesis of 4-Aryltetrahydroisoquinolines
Buev, Evgeny M.,Moshkin, Vladimir S.,Smorodina, Anastasia A.,Sosnovskikh, Vyacheslav Y.
, p. 15307 - 15317 (2021/10/20)
5-Aryloxazolidines react with arenes under Lewis or Br?nsted acid conditions via the Friedel-Crafts/Pictet-Spengler double alkylation sequence to give alkaloid-like 4-aryltetrahydroisoquinolines in 12-94% yields. Three approaches for the controlled insertion of substituents into the target molecules and application of oxazolidine derivatives such as 1-arylethanol-2-amines or 4-hydroxytetrahydroisoquinolines in the alkylation of arenes are also described. An unprecedented two-step easily scalable synthesis of the 4-aryltetrahydroisoquinoline core from aromatic aldehyde was achieved applying oxazolidine methodology.
Method for synthesizing N-methylphenethyl ethanolamine and hydrochloride thereof
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Paragraph 0039; 0045-0058, (2017/08/30)
The invention relates to a method for synthesizing N-methylphenethyl ethanolamine and hydrochloride thereof, and belongs to the technical field of organic synthesis. The method comprises the following steps: dissolving styrene and sodium chloride in a mixed solvent, sequentially adding sulfuric acid aqueous solution and sodium periodate at negative 5-5 DEG C, heating and stirring to react, adding a sodium thiosulfate aqueous solution for a quenching reaction, regulating the pH value to be 8, extracting and concentrating to obtain intermediate (I); adding a methylamine aqueous solution into a reaction bottle, slowly dropwise adding the intermediate (I) into the reaction bottle, stirring overnight at room temperature, performing HPLC detection reaction, and concentrating at reduced pressure to obtain the N-methylphenethyl ethanolamine. In the method for synthesizing N-methylphenethyl ethanolamine, raw materials have low price and are easily available, a low-price conventional reagent is adopted as the reagent, so that the method has low synthesizing cost, mild reaction condition and high conversion rate; and the prepared N-methylphenethyl ethanolamine and hydrochloride thereof have high yield and high purity, and have high quality.
