Synthesis method of ibuprofen caffeate and its application in preparation of immunosuppressive drugs

A synthesis method and caffeic acid ester technology are applied in the synthesis of ibuprofen caffeic acid ester and the application field of preparing immunosuppressive drugs, which can solve the problems such as the unexplained anti-tumor mechanism of ibuprofen, and achieve convenient industrial transformation and inhibition. Proliferation, simple effect
CN111087301BActive Publication Date: 2022-05-20HENAN UNIV OF CHINESE MEDICINE
3 Cites 0 Cited by

Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
HENAN UNIV OF CHINESE MEDICINE
Publication Date
2022-05-20

Smart Images

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

Abstract

The invention discloses a synthesis method of ibuprofen caffeate and its application in the preparation of immunosuppressive drugs. The ibuprofen, anhydrous dichloromethane and pyridine are slowly added dropwise with SOCl under stirring at room temperature. 2 CH 2 Cl 2 Solution, oil bath temperature 55-65 ° C reflux for 2 hours, spin dry, add anhydrous dichloromethane to obtain the CH of ibuprofenyl chloride 2 Cl 2 Solution; cool caffeic acid, DMF and anhydrous dichloromethane in an ice-water bath to 5°C, add triethylamine dropwise, and slowly add CH of ibuprofenyl chloride dropwise under stirring 2 Cl 2 The solution was stirred and reacted in an ice-water bath for 2 h, followed by TLC to detect the reaction to obtain ibuprofen caffeate. The ibuprofen caffeate (CI) provided by the present invention detects its cytotoxicity by the MTT method, and the results show that the inhibitory situation of CI to the proliferation of MCF-7 cells and the proliferation of HepG2 cells is very significant; Induces apoptosis and inhibits proliferation.
Need to check novelty before this filing date? Find Prior Art

Description

technical field

[0001] The invention belongs to the technical field of organic synthesis, and in particular relates to a method for synthesizing ibuprofen caffeate and its application in preparing immunosuppressive drugs. Background technique

[0002] Since the structure of salicylic acid was discovered in willow bark, it has been clinically used for many years including non-steroidal anti-inflammatory drugs (NSAIDs) such as aspirin and ibuprofen. Their main mode of action is to inhibit cyclooxygenase (ie, COX-1 and COX-2) leading to a reduction in the synthesis of prostaglandins (messenger molecules in the inflammatory process), thereby achieving analgesic and anti-inflammatory effects. Ibuprofen has been used clinically for many years and is the most widely applicable non-steroidal drug. It can be used to treat general antipyretic and analgesic as well as rheumatoid arthritis and neuritis.

[0003] A large number of reports have focused on the research of NSAIDs on tumors...

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