125802-07-5Relevant academic research and scientific papers
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
supporting information, 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.
BACE-2 INHIBITORY COMPOUNDS AND RELATED METHODS OF USE
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, (2017/05/02)
Provided herein are novel compounds of Formulae I-III, and methods of using the same to selectively inhibit BACE2.
SUBSTITUTED UREA AND CARBAMATE, PHENACYL-2-HYDROXY-3-DIAMINOALKANE, AND BENZAMIDE-2-HYDROXY-3-DIAMINOALKANE ASPARTYL-PROTEASE INHIBITORS
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Page/Page column 215; 233, (2010/02/14)
The invention relates to acetyl 2-hydroxy-1,3-diaminospirocyclohexanes and derivatives thereof that are useful in treating at least one disease, disorder, and condition associated with amyloidosis. Amyloidosis refers to a collection of diseases, disorders, and condition associated with abnormal deposition of A-beta protein.
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.
Synthesis and Anticonvulsant Activity of 1-Phenylcyclohexylamine Analogues
Thurkauf, Andrew,Costa, Brian de,Yamaguchi, Shun-ichi,Mattson, Mariena V.,Jacobson, Arthur E.,et al.
, p. 1452 - 1458 (2007/10/02)
Thirty-eight analogues of 1-phenylcyclohexylamine (PCA), a phencyclidine (PCP) derivative, were examined for their activities in the mouse maximal electroshock (MES) seizure test and in a motor-toxicity assay.In addition, we determined the binding affinities of the compounds for PCP acceptor sites in rat brain membranes labeled with -1-piperidine.Many of the analogues were protective against MES seizures (ED50s of 4-41 mg/kg, ip) and all of these compounds caused motor toxicity.The potencies in the motor toxicity and MES seizure tests showed a moderate correlation with the affinities for PCP sites.Several analogues exhibited a greater separation of potencies in the motor toxicity and MES seizure tests than did the parent compound PCA.These were obtained by (i) 3-methylation of the cyclohexyl ring trans to the phenyl ring, (ii) methoxylation at the ortho position on the phenyl ring, and (iii) contraction of the cyclohexane ring to form the corresponding cyclopentane.
