Preparation method of 6-(3-chloropropyl)amino-1,3-dimethyluracil

A technology of dimethyluracil and dimethyluracil, which is applied in the field of preparation of 6-amino-1,3-dimethyluracil, can solve the pressure of increasing the cost of labor protection and environmental protection, and increase the synthesis of drugs And drug quality analysis cost, human and environmental hazards and other issues, to achieve the effect of cheap raw materials, green and safe synthesis process, and cost reduction
CN113402469AInactive Publication Date: 2021-09-17沈阳信康药物研究有限公司
2 Cites 0 Cited by

Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
沈阳信康药物研究有限公司
Publication Date
2021-09-17
Estimated Expiration
Not applicable · inactive patent

Smart Images

  • Figure 1
    Figure 1
  • Figure 2
    Figure 2
  • Figure 3
    Figure 3
Patent Text Reader

Abstract

The invention belongs to the technical field of drug synthesis processes, and provides a preparation method of 6-(3-chloropropyl)amino-1,3-dimethyluracil. 6-(3-hydroxypropyl)amino-1,3-dimethyluracil is used as a raw material, and 6-(3-chloropropyl)amino-1,3-dimethyluracil is obtained by chlorination with thionyl chloride. According to the reaction, thionyl chloride is directly used as a reaction reagent and solvent, the yield can reach 85% or above, the highest yield can reach 90% or above, and the highest purity can reach 98% or above. Compared with the prior art, the method has the advantages that the yield and the purity are obviously improved, the post-treatment is convenient, the post-treatment solvent can be recycled, and more importantly, the use of 1,2-dichloroethane which is carcinogenic and harmful to human and environment is avoided. When the method is used for synthesizing an antihypertensive drug urapidil, not only are the types of solvents reduced, but also the analysis of a 1,2-dichloroethane residual solvent in the drug quality analysis is avoided, and the method is a green and safe preparation method which is very suitable for industrial production.
Need to check novelty before this filing date? Find Prior Art

Description

technical field

[0001] The invention belongs to the technical field of medicine synthesis technology, and in particular relates to a preparation method of 6-(3-chloropropyl)amino-1,3-dimethyluracil. Background technique

[0002] 6-(3-Chloropropyl)amino-1,3-dimethyluracil is a very important intermediate in the synthesis of antihypertensive drug urapidil.

[0003] The chemical structure of urapidil is not similar to that of prazosin. It has the effect of blocking postsynaptic receptors and blocking peripheral α2 receptors, but the former is the main one. In addition, it has the effect of activating the central serotonin 1A receptor, which can reduce the sympathetic feedback of the medullary cardiovascular regulation center and play a role in lowering blood pressure. The relaxation effect of this product on veins is greater than that on arteries, and it does not affect intracranial blood pressure when lowering blood pressure. This product can still reduce cardiac preload and...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More