Preparation method of cilnidipine

A technology of cilnidipine and crotonic acid, which is applied in the field of compound synthesis, can solve the problems of increasing the impurity content, long reaction time, increase reaction cost and the like, and achieve the effects of improving purity and yield, short reaction time and less impurities
CN112375031AActive Publication Date: 2021-02-19BENGBU BBCA MEDICINE SCI DEV
5 Cites 0 Cited by

Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
BENGBU BBCA MEDICINE SCI DEV
Publication Date
2021-02-19

Smart Images

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

Abstract

The invention relates to a preparation method of cilnidipine. The invention provides a preparation method of cinnamyl 3-aminobut-2-enoate, which comprises the following step: carrying out amination reaction on cinnamyl acetoacetate and ammonium carbonate to obtain the cinnamyl 3-aminobut-2-enoate. On the basis, the invention further provides a method for preparing cilnidipine by taking the cinnamyl 3-aminobut-2-enoate as a raw material. The method provided by the invention is relatively low in reaction temperature, relatively short in reaction time, relatively high in product yield and purity,and simple in aftertreatment.
Need to check novelty before this filing date? Find Prior Art

Description

technical field

[0001] The invention belongs to the technical field of compound synthesis, and relates to a preparation method of cilnidipine. Background technique

[0002] Cilnidipine is a lipophilic dihydropyridine calcium antagonist used for the treatment of hypertensive patients, and its structural formula is:

[0003]

[0004] In the current technology, the production process of preparing the cinnidipine intermediate amide (cinnamyl 3-amino-2-butenoate) generally adopts cinnamyl acetoacetate dissolved in ethanol to react with ammonia gas at a low temperature of 0-5°C. After the reaction ends, 70°C vacuum distillation; because the reaction generates a molecule of water and the cilnidipine aminate is unstable, it is easy to degrade during vacuum distillation, resulting in more quality impurities in the final cilnidipine product; at the same time, the reaction needs to be controlled less The reaction temperature indirectly increases the reaction cost.

[0005] Simulta...

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