Professor Jiao Ning's research team of Peking University has made important progress in selective functionalization of alcohols
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Last Update: 2018-07-17
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Source: Internet
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Author: User
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Recently, the Journal of naturecommunications published the latest research results of Professor Jiao Ning's research team in the State Key Laboratory of natural and Biomimetic Drugs Online: "silver catalyzed remote csp3-h functionality of aliphatic alcohols" Steroids play an important regulatory role in the body In 2016, the global sales of steroids exceeded US $100 billion, which is the second largest category of chemicals after antibiotics At present, the development of new resources of steroid hormone drugs has been regarded as one of the directions and emphases of the recent development of pharmaceutical industry in China In the synthesis of steroids, the selective functionalization of alcohols (Barton nitrite ester reaction, 1960), developed by Barton, a Nobel Prize winner in 1969, is one of the most important and widely used methods However, Barton reaction requires the pre activation of alcohol, and the activation reagent used in Barton reaction is easy to decompose and has great toxicity How to develop direct selective functionalization of alcohols is a challenging problem in synthetic chemistry for many years Recently, the research team of Jiaoning has achieved a breakthrough by using common silver nitrate as catalyst and sulfonyloxime ether as functional reagent Under the mild conditions without pre activation of alcohol, selective functionalization of alcohol can be achieved in one step The sulfonyloxime ether group can also be further modified to obtain compounds with potential drug activity This method is used to synthesize compounds with antifungal activity In addition, the oxime ether functional group can be transformed into oxadiazole structure by simple transformation This structure is an important pharmacophore in 5-HT1D receptor antagonists and anti scar molecules These transformations are expected to bring more choices for the discovery of drug-induced compounds Zhu Yuchao, a 2016 doctoral student, is the first author of this paper The research is supported by the 973 Program of the Ministry of science and technology and the key program of NSFC.
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