125802-09-7Relevant articles and documents
Synthesis method of six-membered ring benzylamine compound
-
, (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 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.