- Synthetic process improvement method of hydroxypiperidone free alkali
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The invention provides a preparation method for improving the conversion rate of improved hydroxypiperidone free alkali. The method comprises the following step: reacting 2-hydroxypyridine with an epoxy substance shown as a formula I in an organic solvent under the action of a phase transfer catalyst and inorganic alkali to obtain the hydroxypiperidone free alkali shown as a formula II. Accordingto the preparation method, the reaction efficiency is greatly improved, the reaction time is shortened, the reaction yield is increased, and the preparation method is very suitable for industrial production.
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Paragraph 0027-0036
(2020/10/20)
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- Deuterated antidepressant medicine
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The invention provides a compound represented by a structural formula I and a non-toxic pharmaceutically acceptable salt and use thereof in preparation of medicine for treatment of depression. In theformula I shown in the description, R1, R2, R3 and R4 are independent H or deuterium (D) separately, and meanwhile, at least one of the R1, R2, R3 and R4 must be D.
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Paragraph 0009-0010; 0017-0018
(2019/01/23)
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- 1-[(4-HYDROXYPRIDIN-4-YL) METHYL]PYRIDINE-2(1H)-ONE DERIVATIVES, PREPARATION METHODS AND USES THEREOF
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Provided are N-[(4-hydroxypiperidin-4-yl)methyl]pyridin-2(1H)-one derivatives represented by formula I, stereoisomers, pharmaceutically acceptable salts or solvates thereof
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- 1-[(4-hydroxypiperidin-4-yl)methyl]pyridin-2(1H)-one derivatives, preparation methods and uses thereof
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Provided are N-[(4-hydroxypiperidin-4-yl)methyl]pyridin-2(1H)-one derivatives represented by formula I, stereoisomers, pharmaceutically acceptable salts or solvates thereof. The above compounds have the dual activities of 5-hydroxytryptamine 1A receptor ligand and selective serotonin reuptake inhibitor. The preparation methods of the above compounds, the uses of these compounds for the prevention or treatment of nervous system diseases related to 5-hydroxytryptamine system dysfunction and the pharmaceutical compositions containing these compounds are also provided.
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