Compound as well as preparation method and medical application thereof

Abstract

The invention provides a compound and a preparation method and medical application thereof, the compound comprises an acetylcholin esterase inhibitor, and the preparation method comprises the following preparation steps: S1, preparing raw materials including 4-pyridylaldehyde, huperzine B, 10-20 parts of a stabilizer, 5-10 parts of an antioxidant, 6-9 parts of a catalyst, 10-20 parts of purified water, 2-5 parts of a dissolving agent and the like, and mixing together to prepare a substance A; s2, the substance A is placed in a filtering structure to be fully filtered to remove impurities; s3, placing the substance A in a reaction kettle, installing a heating structure, and setting the temperature to be 50-80 DEG C; s4, the reaction time of the substances in the reaction kettle is 5-10 min; s5, filtering and washing the prepared substance; and S6, then drying, storing and using. When the compound is prepared, a stabilizer, an antioxidant and a catalyst are added into the raw materials, so that the compound is fully stirred through a stirring structure during synthesis and reaction, the reaction is sufficient, and the prepared substance can be fully filtered in various modes.

Description

Technical Field

[0001] The present invention relates to the technical field of compound preparation and application, in particular to a compound and a preparation method thereof and medical application thereof. Background Art

[0002] Now, with the increasing severity of aging, more and more people are suffering from Alzheimer's disease. Alzheimer's disease, also known as Alzheimer's disease, is a progressive neurodegenerative disease characterized by dementia such as memory impairment, aphasia, agnosia and behavioral changes, which seriously threatens the health of the elderly. Alzheimer's disease has a high incidence rate, a long course of disease and huge harm. With the intensification of global aging, Alzheimer's disease has become one of the important diseases that the world is concerned about, and it has also become a major public health and scientific issue that affects my country's economic and social development. At present, the most commonly used acetylcholinesterase inhibitor in the clinical treatment of Alzheimer's disease is acetylcholinesterase inhibitor. For the use of acetylcholinesterase inhibitors, it is necessary to set up a compound and its preparation method and medical application.

[0003] With regard to the compounds and their preparation process, the stability of the compounds in the prior art after preparation does not meet expectations and they are easily oxidized. Stirring is performed in a small range during the reaction, so that the reaction sufficiency does not meet expectations. Summary of the invention

[0004] 1. Technical issues to be solved

[0005] In view of the deficiencies in the prior art, the present invention provides a compound and a preparation method and medical application thereof, which solve the problem of easy oxidation and unsatisfactory stability during the preparation process and the problem of insufficient reaction during the preparation process.

[0006] (II) Technical solution

[0007] To achieve the above objectives, the present invention is implemented through the following technical scheme: a compound includes an acetylcholinesterase inhibitor, and the acetylcholinesterase inhibitor includes physostigmine, tetrahydroaminoacridine, donepezil, metrilin and rivastigmine tartrate.

[0008] Preferably, the molecular formula of physostigmine is C 15 H 21 N3O2, the molecular formula of the tetrahydroaminoacridine is C 13 H 15 C l N2.

[0009] A method for preparing a compound, comprising the steps of: S1, preparing raw materials 4-pyridine carboxaldehyde, huperzine B, 10-20 parts of a stabilizer, 5-10 parts of an antioxidant, 6-9 parts of a catalyst, 10-20 parts of purified water, 2-5 parts of a dissolving agent, etc., and mixing them together to prepare substance A;

[0010] S2, placing substance A inside the filtering structure for full filtering and impurity removal;

[0011] S3, placing substance A inside the reactor, installing a heating structure, and setting the temperature to 50-80 degrees Celsius;

[0012] S4, the reaction time of the substance in the reactor is 5-10min;

[0013] S5, filtering and washing the obtained substance;

[0014] S6. Then dry and store for use.

[0015] Preferably, a multi-layer stirring structure is installed inside the reactor, and the stirring structure is divided into a horizontal stirring structure and a vertical stirring structure, and both the horizontal stirring structure and the vertical stirring structure are arc-shaped.

[0016] Preferably, an ultrasonic structure is installed at the upper end of the reaction kettle.

[0017] Preferably, the filtration uses a multi-layer filtration structure with different pore sizes for rotary filtration.

[0018] A compound is used in medicine. The acetylcholinesterase inhibitor is used to treat myasthenia gravis and glaucoma and to resist senile dementia. It is used to treat neurodegenerative diseases. The neurodegenerative diseases are Alzheimer's disease, Parkinson's disease and Lewy body dementia. Patients may experience symptoms such as memory loss, loss of orientation, and mental and behavioral changes.

[0019] (III) Beneficial effects

[0020] The present invention provides a compound and a preparation method and medical application thereof. It has the following beneficial effects:

[0021] When preparing the compound, stabilizers, antioxidants and catalysts are added to the raw materials to make the compound more stable and less prone to oxidation during synthesis, accelerate the reaction catalysis, and fully stir it through a stirring structure during the reaction to ensure sufficient reaction. The obtained substance can be fully filtered and treated in a variety of ways. DETAILED DESCRIPTION

[0022] The following will be combined with the embodiments of the present invention to clearly and completely describe the technical solutions in the embodiments of the present invention. Obviously, the described embodiments are only part of the embodiments of the present invention, not all of the embodiments. Based on the embodiments of the present invention, all other embodiments obtained by ordinary technicians in this field without making creative work are within the scope of protection of the present invention.

[0023] Embodiment 1:

[0024] The embodiment of the present invention provides a compound, including an acetylcholinesterase inhibitor, wherein the acetylcholinesterase inhibitor includes physostigmine, tetrahydroaminoacridine, donepezil, metrilin and rivastigmine tartrate, wherein the chemical name of physostigmine is 1,2,3,3a-hexahydro-1,3a,8-trimethylpyrrolo[2.3-b]indol-5-phenol methylcarbamate, which is an organic compound with a chemical formula of C 15 H 21 N3O2 is a white crystalline powder, slightly soluble in water, easily soluble in ethanol, very soluble in chloroform and dichloromethane, soluble in fixed oil and benzene. Rivastigmine is rivastigmine bitartrate, a Western medicine name. It is an anti-dementia drug. It is used to treat the symptoms of mild and moderate Alzheimer's dementia. The main isomers of tetrahydroaminoacridine are as follows: 1,4,5,8-tetrahydropyridine: melting point 130.5℃, 1,2,3,4-tetrahydropyridine: melting point 55-56℃, its picric acid salt melting point 222℃ decomposition, tetrahydropyridine is hydrogenated to obtain an octahydropyridine mixture; it is condensed with benzaldehyde in the presence of alkali to obtain a 4-benzylidene derivative (melting point 103-104℃). It is condensed with indigo carmine and cyclohexanone in the presence of alkali to generate 1,2,3,4-tetrahydropyridine-9-carboxylic acid, which is then heated to above the melting point for decarboxylation and used in organic synthesis.

[0025] The molecular formula of physostigmine is C15H21N3O2, and the molecular formula of tetrahydroaminoacridine is C13H15C l N2.

[0026] A method for preparing a compound, comprising the steps of:

[0027] S1. Prepare raw materials 4-pyridine carboxaldehyde, huperzine B, 14 parts of stabilizer, 7 parts of antioxidant, 8 parts of catalyst, 13 parts of purified water, 3 parts of solvent, etc. and mix them together to obtain substance A. The antioxidant materials include phenols, hydroxybenzoic acid esters, and diphenols. The stabilizers include phosphites, thiols, and pentaerythritol ethers.

[0028] S2, placing substance A inside the filtering structure for full filtering and impurity removal;

[0029] S3, placing substance A inside the reactor, installing a heating structure, and setting the temperature to 60 degrees Celsius;

[0030] S4, the reaction time of the substance in the reactor is 5-10min;

[0031] S5, filtering and washing the obtained substance;

[0032] S6. Then dry and store it for use. Use a drying fan and drying paper when drying.

[0033] A multi-layer stirring structure is installed inside the reactor. The stirring structure is divided into a horizontal stirring structure and a vertical stirring structure. Both the horizontal stirring structure and the vertical stirring structure are arc-shaped.

[0034] An ultrasonic structure is installed on the upper end of the reactor, and the ultrasonic structure cooperates with the stirring structure to make the stirring more complete.

[0035] The filtration uses a multi-layer filter structure with different pore sizes for rotational filtration.

[0036] The medical application of a compound, acetylcholinesterase inhibitors are used to treat myasthenia gravis and glaucoma and fight senile dementia, and are used to treat neurodegenerative diseases. Neurodegenerative diseases include Alzheimer's disease, Parkinson's disease and Lewy body dementia. Patients may experience symptoms such as memory loss, loss of orientation, and mental and behavioral changes.

[0037] Embodiment 2: A method for preparing a compound, comprising the steps of:

[0038] S1. Prepare raw materials 4-pyridine carboxaldehyde, huperzine B, 17 parts of stabilizer, 9 parts of antioxidant, 9 parts of catalyst, 18 parts of purified water, 4 parts of solvent, etc. and mix them together to obtain substance A;

[0039] S2, placing substance A inside the filtering structure for full filtering and impurity removal;

[0040] S3, placing substance A inside the reactor, installing a heating structure, and setting the temperature to 70 degrees Celsius;

[0041] S4, the reaction time of the substance in the reactor is 5-10min;

[0042] S5, filtering and washing the obtained substance;

[0043] S6. Then dry and store it for use. Use a drying fan and drying paper when drying.

[0044] Although embodiments of the present invention have been shown and described, it will be appreciated by those skilled in the art that various changes, modifications, substitutions and variations may be made to the embodiments without departing from the principles and spirit of the present invention, and that the scope of the present invention is defined by the appended claims and their equivalents.

Claims

1. A compound comprising an acetylcholinesterase inhibitor, characterized in that: The acetylcholinesterase inhibitors include physostigmine, tetrahydroaminoacridine, donepezil, metrilin and rivastigmine tartrate.

2. A compound according to claim 1, characterized in that: The molecular formula of physostigmine is C 15 H 21 N3O2, the molecular formula of the tetrahydroaminoacridine is C 13 H 15 C l N2.

3. A method for preparing a compound, characterized in that: The preparation steps include: S1. Prepare raw materials 4-pyridine carboxaldehyde, huperzine B, 10-20 parts of stabilizer, 5-10 parts of antioxidant, 6-9 parts of catalyst, 10-20 parts of purified water, 2-5 parts of solvent, etc. and mix them together to obtain substance A; S2, placing substance A inside the filtering structure for full filtering and impurity removal; S3, placing substance A inside the reactor, installing a heating structure, and setting the temperature to 50-80 degrees Celsius; S4, the reaction time of the substance in the reactor is 5-10min; S5, filtering and washing the obtained substance; S6. Then dry and store for use.

4. The method for preparing a compound according to claim 3, characterized in that: A multi-layer stirring structure is installed inside the reactor. The stirring structure is divided into a horizontal stirring structure and a vertical stirring structure. Both the horizontal stirring structure and the vertical stirring structure are arc-shaped.

5. The method for preparing a compound according to claim 3, characterized in that: An ultrasonic structure is installed on the upper end of the reaction kettle.

6. The method for preparing a compound according to claim 3, characterized in that: The filtration uses a multi-layer filtration structure with different pore sizes for rotary filtration.

7. Use of a compound in medicine, characterized in that: The acetylcholinesterase inhibitor is used to treat myasthenia gravis and glaucoma and to combat senile dementia, and is used to treat neurodegenerative diseases, such as Alzheimer's disease, Parkinson's disease and Lewy body dementia. Patients may experience symptoms such as memory loss, loss of orientation, and mental and behavioral changes.