NTU has developed a new method for synthesizing anti-inflammatory drugs

Naproxen, diclofenac, ibuprofen and other anti-inflammatory drugs are among the most widely used types of drugs in the world. The traditional synthetic methods for these drugs are complicated, expensive and pollute the environment. A few days ago, the research team of Professor Mao Jianyou at the School of Chemistry and Molecular Engineering of Nanjing University of Technology pioneered a new method that used organic photosensitizers and nickel catalysts to synergistically catalyze different halogenated compounds to form anti-inflammatory drug precursors (that is, the basis for the synthesis of a certain drug). Raw materials). The reaction is easy to operate and low in cost, and provides a convenient and effective synthesis method for the innovative synthesis of anti-inflammatory drugs. The research results were published recently in "German Applied Chemistry".

"Compared with the traditional synthesis method, this method has simple and easily available raw materials, simple operation, simple synthetic route, and low reaction cost, which provides a possible development path for subsequent industrial production applications." Professor Mao Jianyou introduced that in the traditional method Organometallic reagents (format reagents, organozinc reagents, organosilicon reagents, organoboron reagents, etc.) will be used. Among them, the format reagent and the organic zinc reagent are very sensitive to air and water, and are flammable and explosive reagents. In the process of use, a little carelessness will cause fire and explosion. Therefore, the requirements for operation during their use are extremely high; ; And the use of reducing metals (zinc powder, manganese powder, magnesium scraps, etc.) will not only cause wear on the experimental instrument, thereby shortening the service life of the instrument, but also cause repeated experiments due to different objective factors such as batch and origin. In addition, the generation of metal salt waste will also pollute the environment.

"Our research team used an organic photosensitizer and a nickel catalyst to synergistically catalyze the reaction of two different halides (iodide and chloride) to produce an anti-inflammatory drug precursor." The first author of the paper, a doctoral student at Nanjing University Guan Haixing stated that this reaction not only avoids the use of organometallic reagents (halogens replace the use of organometallic reagents), but also avoids the use of reducing metals (photosensitizers replace the use of reducing metals); at the same time The organic photosensitizer and alkali used in the reaction can also be recycled repeatedly, which also greatly reduces the reaction cost and provides potential for further industrialization.

Professor Mao Jianyou introduced that halogenated compounds are easy to obtain and are one of the most important raw materials in the field of organic synthesis. In the next step, they will continue to work on synergistic catalytic strategies using photosensitizers and nickel catalysts, select different halogenated compounds for reaction, and thus develop new methods for synthesizing chiral drug precursors, which will be applied to more valuable framework structures ( In the synthesis of the precursor of a drug).