95425-81-3Relevant academic research and scientific papers
Polysubstituted ethylene compound as well as preparation method and application thereof
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Paragraph 0125-0129; 0285-0289, (2020/12/30)
The invention discloses a polysubstituted ethylene compound as well as a preparation method and application thereof. The invention particularly discloses a preparation method of a polysubstituted ethylene compound as shown in a formula III, which comprises the following step: in an organic solvent, carrying out reaction as shown in the specification on a compound as shown in a formula I and a compound as shown in a formula II in the presence of a palladium catalyst, a phosphine ligand and alkali to obtain the polysubstituted ethylene compound as shown in the formula III. The preparation methodcan be suitable for various types of substrates, and the configuration of double bonds is controllable.
Compound having dual effects on 5-HT and application thereof in treatment of depression
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Paragraph 0028; 0035; 0036; 0037, (2018/09/21)
The invention discloses a compound having dual effects on 5-HT and application thereof in treatment of depression. As shown in the description, R1, R2, R3 and R4 are independently selected from H, F or CH3. In recent years, a dual-effect anti-depression drug with partial excitation of serotonin 1A receptor and selective serotonin reuptake inhibition becomes a hot spot for new antidepressant research. In rat synaptosome, [3H]5-HT uptake inhibition and h5-HT1A binding affinity experiments prove that the compound has 5-HT reuptake inhibition effect and 5-HT1A receptor excitation effect, indicating that the compound can be used as a medicament for treating central nervous system dysfunction such as depression and anxiety in humans.
Compound having dual functions to 5-HT and application thereof in depressive disorder treatment
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Paragraph 0028; 0035-0037, (2018/10/19)
The invention discloses a compound having dual functions to 5-HT and application thereof in depressive disorder treatment. The formula is shown in the description, wherein R1, R2, R3 and R4 are independently selected from H, F or OH. In recent years, an antidepressant having the dual functions of 5-hydroxytryptamine 1A acceptor partial agitation and selective 5-hydroxytryptamine re-uptake inhibition becomes a hot point direction of a novel antidepressant drug research. In a [3H]5-HT uptake inhibiting effect experiment of a rat synaptosome and a h5-HT1A combined affinity experiment, the compound is verified to have the 5-HT re-uptake inhibiting effect and the agitating effect to a 5-HT1A acceptor. The fact that the compound can be used as a drug for treating human central nervous system disorders, such as a depressive disorder and an anxiety disorder, is demonstrated.
