5029-76-5Relevant academic research and scientific papers
A green synthetic benproperine phosphate in intermediates (by machine translation)
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Paragraph 0019; 0020; 0021, (2018/11/22)
A green synthetic benproperine phosphate in intermediates, which belongs to the technical field of pharmaceutical intermediates. The process in the phenol and benzyl alcohol benzylating reaction, the introduction of 1, 1, 3, 3 - [...] sulfonyl propylene (TTP)/hexafluoroisopropanol (HFIP) catalytic system, the steps of reaction to enhance the yield of 95% - 100%; after a series of reaction can obtain the target product benproperine phosphate, avoid the Al2 O3 First activated and reaction, the production process is greatly simplified, improving the selectivity, yield is greatly improved. In the substituted hydroxy substitution chlorine in the step into, the introduction of methyl dichloro silane, anhydrous ferric trichloride, ethylene glycol dimethyl ether replacing thionyl chloride, benzene and pyridine. No sulfur dioxide, hydrogen chloride and other corrosive contaminants. Reduces the environment pollution and difficulty of post-processing; and easy operation, processing is simple. The method greatly improves the yield, the cost is reduced, and the safety is improved, and the energy is saved, accord with the green reaction of modern chemical production requirement. (by machine translation)
COMPOSITION COMPRISING BENPROPERINE DERIVATIVES AS ACTIVE INGREDIENTS FOR PREVENTING AND TREATING ANGIOGENESIS-RELATED DISEASES
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Paragraph 0067; 0068, (2013/09/26)
The present invention relates to a novel pharmaceutical composition of benproperine derivatives for preventing and treating angiogenesis-related diseases. The benproperine derivatives and pharmaceutically acceptable salts thereof according to the present invention inhibit cancer cell migration and the angiogenesis of vascular endothelial cells, and therefore can be effectively used not only as an anticancer agent, but also as an agent for preventing and treating diseases caused by abnormal angiogenesis, such as diabetic retinopathy and corneal transplant rejection.
