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Angew.Chem.Int.Ed.2015,54,656~659自然界的生命过程完全不依赖氟的代谢,因而含氟的有机化合物在自然界中的含量微乎其微.然而,目前很多药物分子中都含有至少一个氟原子,主要是因为氟原子的存在可以改变药物分子的脂溶性和代谢稳定性等.如何不对称构筑C—F键,是有机氟化学中的一个难点.清华大学医学院药学系汪舰课题组首次报道了一种通过氮杂卡宾催化,N-氟代双苯磺酰胺(NFSI)氧化,在简单脂肪醛的α-位不对称氟化的方法.N-氟代双苯磺酰胺(NFSI)是工业上常用的氟试剂,市场上广泛易得,但是其作为氧化
Angew.Chem.Int.Ed.2015,54,656 ~ 659 The life processes of nature do not rely on the metabolism of fluorine at all, so the contents of fluorine-containing organic compounds are negligible in nature.However, at present, many drug molecules contain at least one fluorine atom , Mainly due to the existence of fluorine atoms can change the lipid solubility and metabolic stability of drug molecules, etc. How asymmetric building C-F bond is a difficult organofluorine chemistry Department of Pharmacy, Tsinghua University, Wang Shiping group for the first time A method of asymmetric fluorination at the α-position of simple aliphatic aldehydes by N-fluorobisbenzenesulfonamide (NFSI) oxidation by azaborine is reported N-fluorobisbenzenesulfonamide (NFSI) is Fluorine reagents commonly used in the industry are widely available on the market, but they are used as oxidation