He has been engaged in scientific research for more than 50 years, which has played a positive role in promoting the development of natural product chemistry in China. Especially, important achievements have been made in the research of tumor chemotherapy drugs (plant growth hormone analogues) and the total synthesis of natural products.
Chinese Name: Gao Yisheng Nationality: China Birthplace: Nanjing Date of Birth:1910 Date of Death:1992 May 30 Occupation: Pharmaceutical Chemist Graduate School: Department of Chemistry, National Central University (now Nanjing University) Major Achievements: Representative of Chinese Academy of Sciences: chlorine. Biography, personal life, major contributions, tumor chemistry, synthesis of natural products, in Lecaiying Institute of Medicine, major works, biographies of people1910 was born in an intellectual family in Nanjing on August 30, 2000, with a large number of books at home, and developed the habit of reading extensively since childhood. After graduating from high school, he was admitted to the Chemistry Department of National Central University (now Nanjing University) with excellent results. From 65438 to 0934, Gao Yisheng completed his graduation thesis "Qualitative Analysis of Steroids" under the guidance of organic chemist Zhuang Changgong, and graduated from the Chemistry Department of National Central University (now Nanjing University). He was recommended as an assistant researcher at the Institute of Chemistry, Academia Sinica, and began his research career in organic chemistry and medicinal chemistry. Under the guidance of Zhuang Changgong, he studied the structure of tetrandrine, a new alkaloid of tetrandrine, and the paper was published in the Journal of the German Chemical Society. From 65438 to 0940, he entered the Institute of Pharmacology of National Peking Research Institute with Zhuang Changgong, and continued to engage in the chemical research of natural products. From 1940 to 1945, I worked as a technician in Shanghai Hisense Pharmaceutical Factory and taught chemistry at Nanjing Zhongying Middle School and Nanjing Central University. After War of Resistance against Japanese Aggression's victory, he returned to the Institute of Pharmacology of Beijing Research Institute as an associate researcher and continued to study the chemical constituents of Chinese herbal medicines. From 65438 to 0948, he was funded by the British Council and went to Oxford University for further study. He studied fine organic synthesis under the Nobel Prize winner and famous organic chemist Professor Robinson. /kloc-completed the thesis in 0/950 and obtained the doctorate from Oxford University. Zhuang Changgong returned to China as a researcher in 1950, and soon participated in the establishment of the Institute of Pharmacology of China Academy of Sciences, and served as the deputy director, leading the research work in the fields of medicinal chemistry and natural organic chemistry. 1978 ——1984, director of the institute. He used to be the first director of Shanghai Family Planning Institute, director of Chinese Pharmaceutical Association and chairman of Shanghai Branch, director of chinese chemical society, honorary director of Shanghai Pharmaceutical Institute and honorary chairman of Shanghai Branch of Chinese Pharmaceutical Association. He also serves on the editorial boards of China Science, Science Bulletin, Chemical Journal and Pharmaceutical Journal. 1980 was elected as a member of the Department of Chemistry of China Academy of Sciences. For more than half a century, he has devoted himself tirelessly to the development of pharmacy and natural product chemistry in China and made outstanding achievements. He used to be an assistant researcher in the Institute of Chemistry of Academia Sinica and an associate researcher in the Institute of Pharmacology of Peiping Research Institute, and soon joined the Institute of Pharmacology of China Academy of Sciences as the deputy director, leading the research work in the fields of medicinal chemistry and natural organic chemistry. He won the second prize of National Natural Science Award 1982, and also directed the synthesis of effective components of anti-asthma and effective components of Agrimonia pilosa, such as camptothecin and coriander, and won the third prize of National Natural Science Award 1989, and published more than 70 papers. 1992 died in Shanghai on May 30th. Personal life is high to promote his wife Qin Jingxian. Mrs Qin Jingxian mainly contributed to tumor chemistry. She carried out the research on new synthesis methods of chloramphenicol and its analogues and the work of synthesizing isoniazid from citric acid, which opened up the field of medicinal chemistry for designing and synthesizing new drugs. In terms of tumor drugs, she creatively designed and directed the synthesis of hundreds of compounds, such as camptothecin harringtonine and other analogues. Among more than 2,000 compounds synthesized, 7~8 new anti-tumor drugs have been used in clinic. In natural organic chemistry, the separation, crystallization, structural derivation and total synthesis of several compounds, such as liensinine and jejunic acid, which are effective antihypertensive components, have been completed. At the beginning of 1950 Gao Yisheng's return to China, combined with the actual needs of China's pharmaceutical industry, a new synthesis method of chloramphenicol and its analogues and the research on the synthesis of isoniazid from citric acid were carried out, which opened up the field of medicinal chemistry for designing and synthesizing new drugs by the Institute of Medicine. After 1958, he turned to the study of chemotherapy drugs for tumors, the most serious disease endangering human life, and devoted a lot of effort. The design and synthesis of anti-tumor compounds is a hard and long-term work. When he was engaged in this research, he emphasized that he should not be bound by traditional academic thoughts, but must innovate and go his own way. In 1950s and early 1960s, the synthesis of tumor drugs was generally inseparable from nitrogen mustard compounds. However, these drugs have poor selectivity to tumor cells and great toxicity to human body. He actively advocated jumping out of the nitrogen mustard circle and trying to synthesize some plant growth hormone analogues to observe their inhibitory effects on tumor cells. He believes that plant growth hormone has a selective effect on plant cells, while animals and plant cells are basically similar, so plant growth hormone may also have a selective inhibitory effect on tumor cells in animals. On this basis, he designed and guided young researchers to synthesize a series of plant growth hormone analogues, among which several compounds have inhibition rates of 70%-80% on sarcoma 180 and sarcoma 57. He also led the synthesis of many natural anti-tumor drugs, such as camptothecin, harringtonine and other analogues, some of which have stronger anti-tumor effects than the original natural products. Among more than 2,000 compounds synthesized under his leadership, after screening, rigorous pharmacological tests and clinical verification, seven or eight compounds have been approved as new anti-tumor drugs, such as methoxyaromatic mustard seed, and some of them are still in clinical application. It is very interesting for organic chemists to synthesize bioactive components in traditional medicines from natural products, from which new compounds with unique structures can often be found. In recent 40 years, China has done a lot of work in this field. There are hundreds of effective components of Chinese herbal medicine that have been separated, purified and clarified, many of which have been produced in pharmaceutical factories and used for clinical treatment of various diseases. However, the total synthesis of natural products is rarely carried out. Gao Yisheng believes that the chemical research of natural products should not be limited to separation and crystallization, but should deduce the structure, plus overall synthesis, so that the whole research work can form a whole. Since the late 1950s, he has actively advocated the steady development of this systematic work and put it into practice. Under his leadership, he has successively completed the systematic work of separation, crystallization, structural derivation and total synthesis of many compounds, such as liensinine, the effective component of lotus plumule for lowering blood pressure, quisqualine, the effective component of traditional Chinese medicine for expelling insects, and chalcone, the effective component of licorice. In 1970s and 1980s, he also directed the synthesis of effective antiasthmatic components, such as POTAMOGETON POTAMOGETON, Agrimonin and natural anticancer drugs, such as camptothecin and hydroxycamptothecin. His research on the active components of twelve Chinese herbal medicines won the second prize of the National Natural Science Award 1982. Later, he started the total synthesis of maymenine, an effective anticancer component, which was more difficult to synthesize. In this work completed in 1986, he not only absorbed the experience of predecessors, but also incorporated his own new ideas into the design of synthetic routes. For example, in the key step of the closed-loop reaction, he applied the reagent 1- methyl -2- bromopyridine iodide to the synthesis of macrolactams, and achieved ideal results. This work won the second prize of 1988 China Academy of Sciences and the third prize of 1989 National Natural Science Award. In addition, fully aware of the strategic significance of family planning, he served as the director of Shanghai Family Planning Institute in 1980- 1983, and personally presided over the major scientific research project of human family planning of the World Health Organization. During this period, he attached great importance to the research work of using the advantages of Chinese herbal medicine resources to find new, effective and safe family planning drugs. For example, with his advice and support, the comrades concerned isolated a variety of effective antifertility compounds from plants such as Hibiscus pseudolaricis, Daphne genkwa and Gardenia, and completed related chemical work. From 65438 to 0952, Gao Yisheng, deputy director of Shanghai Institute of Pharmacology, Chinese Academy of Sciences, assisted Mr. Zhao Chengyu, director of the Institute, and made a long-term plan for the main attack direction, specialty setting and personnel training of the Institute, and put them into practice one by one. Prior to this, the focus of medicine was phytochemistry, mainly the separation, extraction and structural identification of Chinese herbal medicine components. He and Zhao Chengtuo realized that the extraction of Chinese herbal medicine components must be effectively coordinated through pharmacological experiments, and phytochemistry and synthesis methods should not be neglected. They are keenly aware that in China, for a period of time, it is difficult for pharmaceutical companies to undertake the task of developing innovative drugs themselves, and they must obtain the support of professional research institutions. Therefore, the Institute of Pharmacology should make due contributions in this respect. Under the guidance of these ideas, they vigorously recruited talents and extended their disciplines, and successively set up laboratories for pharmacology, synthesis, analysis and antibiotics in a relatively short period of time. Especially during the period from 1978 to 1984, under the situation of reform and opening up, he sent a large number of young and middle-aged scientific research backbones to Europe and America for further study. Encourage and support senior researchers to participate in international conferences, obtain information and expand their influence; Vigorously carry out international cooperation and purchase instruments and equipment, so that the academic atmosphere in the hospital is strong and the backbone grows rapidly. Over the past decades, the Institute of Medicine has been developing continuously, and now it has become a new drug research institution closely combining chemistry and biology, enjoying a certain reputation at home and abroad, and has developed a number of new drugs that are effective in tumor, cardiovascular, neurological and parasitic diseases, such as common morpholine, bimorphine, butorphanol, tetrahydropalmatine, huperzine A and artemether, which have made beneficial contributions to the development of new drugs in China. Zhao Chengyu likes educating people, fears life, fears learning and is strict with himself. He guides students, not only in topics, design, etc., but also has strict requirements on the progress of daily work. For the specific experimental process, he asked for careful observation and detailed records; If the experiment fails, we must carefully analyze the real reason for the failure. He is not allowed to change the design route easily before there is enough evidence to show that the reaction cannot be carried out or the expected results cannot be obtained. His students may not be used to such strict requirements at that time, but after several years, they all sincerely feel that his strict requirements have played a great role in their progress. Since 1950s, a group of college students or graduate students who are afraid of students for the country have grown into leading backbones and academic leaders, and the third generation of young scientists have been trained through them. His rigorous style has also been passed down from generation to generation, becoming the traditional style of the Institute of Medicine. For more than half a century, Gao Afraid students have published more than 70 papers, which have been reprinted and quoted by relevant foreign monographs for many times, enjoying a good reputation in academic circles at home and abroad. Shanghai Medical Research Institute has bound his papers and displayed them in the reading room. After entering the octogenarian, although he has retired to the second line, he still cares about the research work, always pays attention to the latest progress in international pharmacy and organic chemistry, and puts forward new suggestions at any time, indicating that he will continue to work hard to cultivate new forces, develop China's scientific career, and make new contributions to the benefit of mankind. 1On May 30th, 992, Gao Yisheng died of illness in Shanghai. This paper mainly discusses 1 high to rise. Two kinds of α-(2- pyridyl)-β-alkyl indanes? And the synthesis of several derivatives of carbaryl. Chinese Journal of Chemistry,1955,21:159—167; 2 Gao Yisheng, Pan Baichuan, Lu Shunxing, et al. Synthesis of useful intermediates for the preparation of chloramphenicol and some related condensation reactions, Journal of Chemistry, 1956, 22: 24-32; 3 high to rise. Present situation and development trend of medicinal chemistry. Science bulletin, 1956, 40-45.4 Gao Yisheng, Dae-kun Lee. Synthesis of chloramphenicol compound I, 3- (o-chloroacetyl-p-nitrophenyl)-propanol. Journal of Chemistry, 1956, 22: 33-38.5, Gao Yisheng. 6 Gao Yisheng, Xu Xiurong, Chen Zhihao, et al. Preparation of several β-methoxyphenylacetone from Mannig base. Journal of Chemistry, 1957, 23: 385-390; 7 high to rise. Hydrogen peroxide on 2- methyl -3-(β- diethylamino)-indane? Journal of Chemistry,1957—23: 287—290; 8 Gao Yisheng, Xu Xiurong. Synthesis of chloramphenicol compounds ⅲ. 1- (o-hydroxy p-nitrobenzene) -2- dichloroacetamide ethanol and 1- (o-hydroxymethyl p-nitrobenzene) -2- dichloroacetamide ethanol. Journal of chemistry, 1958, 24: 6548. 9 Speak louder, Pan Baichuan. Synthesis of organic compounds with hydrogen bonds in their molecules Ⅱ. α-Dichloroacetamido-β-hydroxy-o-p-nitrobenzone and its related compounds. 10 Weng Zunyao, high to rise. Synthesis of 1- phenyl. 1, 3- propanediol and other 65438+ were reacted by W0hl-Eiegler. 1 1 high to rise. Present situation and prospect of antineoplastic chemotherapy. Science bulletin,1960:129-132.12 is one liter higher, Pan Baichuan. Synthesis of chloramphenicol ⅳ. 3- (o-hydroxy p-nitrophenyl) -2. 13 Pan Baichuan, Zhou? Li, Gao Yisheng, et al. Studies on alkaloids from plumula nelumbinis Ⅱ. Structure of nuciferine. 1962:11:321-336.14 mo, a long life. Chemotherapy of tumor XXXVI. Some 1- ethyl. Synthesis of 4- tetrahydrophenanthrene -2- carboxylic acid and 2- napropionic acid. Journal of Chemistry, 1978, 36: 297-306. 15 Zhang Hongliang, Qu Chongjie, Gao Yisheng, et al. Chemotherapy of tumor. Synthesis of several plant growth regulator derivatives and their antitumor effects. Acta pharmacy, 6548. 14: 302—308. 16 Xu rensheng, Xie yuyuan, Gao Yisheng, etc. Isolation, structure and total synthesis of chalcone from Glycyrrhiza uralensis Fisch Journal of Chemistry, 1979, 37: 289—297. 17 Gao Yisheng. Organic synthesis of phytochemistry. 2 1: 7579. 18 Gao Yisheng, Xu Rensheng, Xie Yuyuan. Some advances in chemical research of Chinese herbal medicine. Chemical bulletin, 1979,11-21.19 Pan Baichuan, Zhang Hong. 1980, 38: 502-506.20 Zhou Qiting, Bai Donglu, Gao Yisheng, et al. Study on the total synthesis of maytansinone Ⅱ. Synthesis of C9-N fragment. Journal of Chemistry, 1980, 38: 507-510.50086.100666666661985: 265438+24 Gu Xueqin, Pan Baichuan, Gao Yisheng, et al. Synthesis of C5-N fragment. Zhongke Series B,1987:12941300; Gu Xueqin, Pan Baichuan, Gao Shen Sheng, etc. Study on total synthesis of maytansinone ⅳ. Synthesis of maytansine. China Science Series B,1987:1301-1308.