The first high efficient synthetic method of artemisinin in China

On July 4, the reporter learned from Shanghai Jiaotong University that the scientific research team led by Professor Zhang Wanbin, after seven years and numerous experiments, finally developed a conventional chemical synthesis method, which realized the high-efficiency artificial synthesis of the antimalarial drug artemisinin for the first time, enabling artemisinin to achieve large-scale industrial production, benefiting hundreds of millions of patients In the 1970s, Chinese scientists first discovered that artemisinin was used to treat malaria, which made the global medical community happy However, it has been found that how to synthesize artemisinin efficiently and form large-scale production has become a worldwide problem Decades on, scientists all over the world have worked hard to solve the problem, but little has been achieved Because of the low content of artemisinin in natural plants, the production cost of artemisinin is very high and the price of artemisinin is expensive According to the statistics of the World Health Organization, there are 300-500 million people infected with malaria every year in the world, and nearly 1 million people die due to the lack of effective drug treatment Professor Zhang Wanbin introduced that at present, artemisinin sources are all extracted from the traditional Chinese medicine Artemisia annua 80% of the world's raw material Artemisia is from Youyang, Chongqing, China, and the output of Artemisia is greatly affected by the environment and weather At the same time, the cultivation of Artemisia annua needs a large area, consumes a lot of organic solvents, and produces a lot of waste, resulting in serious waste of land and material resources Can chemical synthesis be used to produce artemisinin in large quantities? Scientists at home and abroad have also made a lot of attempts, but so far there is no report of industrial production Since the early 1980s, academician Zhou Weishan and researchers of Novartis in Switzerland have respectively synthesized artemisinin by chemical methods, many famous chemists at home and abroad have carried out chemical synthesis research for more than 30 years, but the yield is low and it is difficult to industrialize Professor Zhang Wanbin has listed a series of figures: one ton of Artemisia annua can extract 6 to 8 kg of artemisinin, which is 4000 to 6000 yuan per kg of artemisinin; in addition, a lot of waste materials are generated, which not only wastes raw materials, but also seriously pollutes the environment Therefore, artemisinin as an important strategic material, its industrial production has always been a challenge for the international pharmaceutical industry Artemisinin is not cheap because it can't be produced on a large scale and its extraction cost is high In order to solve this world problem, the team led by Professor Zhang Wanbin started to carry out research work in this field since 2005 After seven years of exploration and efforts, great progress has been made in the near future Researchers used a specific catalyst they found to reduce artemisinin to dihydroartemisinin, which can be easily and efficiently obtained by a conventional synthesis route without light Then, artemisinin can be obtained in high yield by oxidative rearrangement The synthesis route is short and the yield is high Because there is no need for special chemical reaction conditions such as light, it is suitable for large-scale industrial production The major breakthrough of Professor Zhang Wanbin's achievements lies in that raw materials can be obtained from waste materials of artemisinin extraction or monosaccharide fermentation, and conventional chemical synthesis can be realized by using key catalysts, which is convenient for large-scale and industrial production At the same time, artemisinin was obtained with a high yield of nearly 60%, and the synthesis efficiency was high The results are expected to solve the major problem of artemisinin high-efficiency artificial synthesis that has puzzled the world pharmaceutical industry for more than 30 years, and make artemisinin drugs cheaper and easier to obtain At present, this achievement is ready to apply for an international patent Team members will increase the experimental site as soon as possible, expand the team of R & D personnel, plan the pilot scale-up and industrialization scheme, and accelerate the industrialization process.