CN-121974782-A - Preparation method of anticoagulation activity racemized borneol for diagnosing and treating thrombus

Abstract

The invention discloses a preparation method of anticoagulation activity racemized borneol for thrombus diagnosis and treatment, which comprises the following specific steps of S1, weighing a levo-borneol crystal, a dextro-borneol crystal and white spirit, mixing the levo-borneol crystal, the dextro-borneol crystal and the white spirit, S2, placing the mixture into an autoclave filled with distilled water, continuously cooking the mixture for 4-8 hours by using small fire after the mixture is heated to a boiling state of 100-105 ℃ by using big fire, and S3, cooling and crystallizing the mixture to obtain the racemized borneol.

Inventors

• GU JINGEN
• Gu Qinfang

Assignees

• 顾金根

Dates

Publication Date

20260505

Application Date

20260120

Claims (5)

1. 1. A preparation method of anticoagulation activity racemized borneol for diagnosing thrombus is characterized by comprising the following specific steps of S1, weighing a L-borneol crystal, a D-borneol crystal and white spirit, mixing the L-borneol crystal, the D-borneol crystal and the white spirit, S2, placing the mixture into an autoclave filled with distilled water, continuously steaming with small fire for 4-8 hours after the mixture is heated to a boiling state of 100-105 ℃ by using big fire in the autoclave, and S3, cooling and crystallizing to obtain the racemized borneol.
2. 2. The method for preparing the anticoagulative racemic borneol for thrombus diagnosis and treatment according to claim 1, wherein both the levoborneol and the dextroborneol are medical grade.
3. 3. The method for preparing the anti-coagulant activity racemic borneol for diagnosing and treating thrombus according to claim 1, wherein the degree of white spirit is 60 °.
4. 4. The method for preparing the anti-coagulant activity racemic borneol for diagnosing and treating thrombus according to claim 1, wherein the weight ratio of the L-borneol crystals to the D-borneol crystals to the white spirit in the step S1 is 10:10:3.
5. 5. The method for preparing the anti-coagulation active racemic borneol for diagnosing and treating thrombus according to claim 4, wherein the weight ratio of the mixture to distilled water in the step S1 is 1:1000-8:1000.

Description

Preparation method of anticoagulation activity racemized borneol for diagnosing and treating thrombus Technical Field The invention belongs to the technical field of racemized borneol, and relates to a preparation method of anticoagulation activity racemized borneol for diagnosing and treating thrombus. Background The chemical structure of natural borneol (dextro borneol) is in the form of single dextro enantiomer, which is mainly extracted from borneol camphor plant, and the purity of the borneol is generally more than 98 percent. Clinical researches show that the composition has a certain protection effect on cerebral ischemia and myocardial tissue, but the effect is superior to Ai Pianlve on one hand. The blumea balsamifera tablet belongs to a levorotatory single enantiomer compound, is mainly extracted from blumea balsamifera plants of the Compositae, and has the purity of more than 96 percent. In clinical applications, it exhibits a comprehensive and remarkable protective effect in cerebral ischemia and acute myocardial infarction. Based on this property, "warfarin" has developed and its active ingredient (API) synthesis aims to prepare warfarin molecules. The classical synthesis route is the one-step synthesis of racemic warfarin acid by the michael addition reaction of 4-hydroxycoumarin with benzalacetone (conventional method). In the prior art, the racemate is synthesized firstly, then chiral reagent (such as quinidine) is used for forming a compound with the racemate, and then the compound is separated through a plurality of complicated recrystallization operations. The method has the disadvantage of larger side effect, and can cause adverse reactions such as dizziness, five sense organs bleeding and the like. Therefore, designing a preparation method of the anti-coagulation activity racemic borneol for diagnosing and treating thrombus has become a key problem to be solved urgently. Disclosure of Invention In order to solve the defects of the prior art, the invention provides a preparation method of the anticoagulation activity racemized borneol for diagnosing and treating thrombus. In order to achieve the aim, the technical scheme of the invention is that the preparation method of the racemic borneol with anticoagulation activity for diagnosing and treating thrombus comprises the following specific steps: S1, weighing the L-borneol crystals, the D-borneol crystals and white spirit, mixing the L-borneol crystals, the D-borneol crystals and the white spirit, S2, placing the mixture into a pressure cooker filled with distilled water, heating the mixture to a boiling state of 100-105 ℃ by using big fire in the cooker, continuously steaming the mixture for 4-8 hours by using small fire, and S3, cooling and crystallizing the mixture to obtain the racemic borneol. Both the L-borneol and the D-borneol are medical grade. The degree of the white spirit is 60 degrees. The weight ratio of the L-borneol crystals to the D-borneol crystals to the white spirit in the step S1 is 10:10:3. The weight ratio of the mixture in the step S1 to distilled water is 1:1000-8:1000. By adopting the technical scheme, the invention has the beneficial effects that: According to the invention, medical grade L-borneol and D-borneol are mixed according to an equal weight proportion, 60-degree white spirit with a specific weight proportion is used as a medium, the mixture is mixed with distilled water in an autoclave according to an accurate proportion, then the mixture is heated to a specific boiling temperature through big fire, and then the mixture is continuously boiled for a plurality of hours through small fire, and finally the mixture is cooled and crystallized, so that the racemic borneol with anticoagulation activity is successfully prepared. The method is simple and convenient to operate, avoids the problems of complicated resolution and larger side effects caused by the chiral reagent in the traditional warfarin synthesis process, provides a new preparation way of anticoagulation active substances with potential application value for thrombus diagnosis and treatment, has mild preparation process conditions, is easy to control, and is expected to reduce the production cost and reduce the occurrence risk of adverse reactions. Detailed Description In order to further explain the technical scheme of the invention, the invention is explained in detail by specific examples. The preparation method of the anticoagulation activity racemized borneol for diagnosing and treating thrombus comprises the following specific steps: S1, weighing the L-borneol crystals, the D-borneol crystals and white spirit, mixing the L-borneol crystals, the D-borneol crystals and the white spirit, S2, placing the mixture into a pressure cooker filled with distilled water, heating the mixture to a boiling state of 100-105 ℃ by using big fire in the cooker, continuously steaming the mixture for 4-8 hours by using small fire, and S3, cooling and crystallizi