125802-07-5Relevant articles and documents
Synthesis method of six-membered ring benzylamine compound
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, (2022/03/27)
The invention relates to the field of synthesis of organic matters, and particularly discloses a synthesis method of a six-membered ring benzylamine compound, which comprises the following steps: taking a compound D, a compound E and potassium tert-butoxide as raw materials, taking dimethyl sulfoxide as a solvent, reacting at 5-10 DEG C for 1-2 hours, heating to 20 DEG C, reacting, and purifying and separating after the reaction is finished to obtain a compound A; the method comprises the following steps: by taking a compound A, potassium carbonate and hydrogen peroxide as raw materials and dimethyl sulfoxide as a solvent, reacting at 50-65 DEG C, adding ice water to separate out a product after the reaction is finished, filtering and washing to obtain a compound B; dissolving the compound B in acetonitrile, adjusting the pH value to 13-14, adding a saturated sodium hypochlorite solution for reaction, and purifying and washing after the reaction is finished to obtain a compound C; the method has the effect of improving the defect that the synthesis process of the six-membered ring benzylamine compound is not suitable for industrial production.
Synthesis of 4H-1,3-Benzoxazines via Metal- and Oxidizing Reagent-Free Aromatic C-H Oxygenation
Xu, Fan,Qian, Xiang-Yang,Li, Yan-Jie,Xu, Hai-Chao
, p. 6332 - 6335 (2017/12/08)
An unprecedented electrochemical aromatic C-H oxygenation reaction for the synthesis of 4H-1,3-benzoxazines from easily available N-benzylamides is reported. These oxidative cyclization reactions proceed in a transition metal- and oxidizing reagent-free fashion and produce H2 as only theoretical byproduct. Adapting the C-H oxygenation reaction in an electrochemical microreactor has been demonstrated.
HYDROXYETHYLAMINE DERIVATIVES FOR THE TREATMENT OF ALZHEIMER'S DISEASE
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Page 76-77, (2010/02/07)
The present invention relates to novel hydroxyethylamine compounds of formula (I): (I) having Asp2 (-secretase, BACE1 or Memapsin) inhibitory activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases characterised by elevated-amyloid levels or-amyloid deposits, particularly Alzheimer's disease.