616214-72-3Relevant articles and documents
A Broad-Spectrum Catalytic Amidation of Sulfonyl Fluorides and Fluorosulfates**
Wei, Mingjie,Liang, Dacheng,Cao, Xiaohui,Luo, Wenjun,Ma, Guojian,Liu, Zeyuan,Li, Le
supporting information, p. 7397 - 7404 (2021/02/16)
A broad-spectrum, catalytic method has been developed for the synthesis of sulfonamides and sulfamates. With the activation by the combination of a catalytic amount of 1-hydroxybenzotriazole (HOBt) and silicon additives, amidations of sulfonyl fluorides and fluorosulfates proceeded smoothly and excellent yields were generally obtained (87–99 %). Noticeably, this protocol is particularly efficient for sterically hindered substrates. Catalyst loading is generally low and only 0.02 mol % of catalyst is required for the multidecagram-scale synthesis of an amantadine derivative. In addition, the potential of this method in medicinal chemistry has been demonstrated by the synthesis of the marketed drug Fedratinib via a key intermediate sulfonyl fluoride 13. Since a large number of amines are commercially available, this route provides a facile entry to access Fedratinib analogues for biological screening.
Efficient Enantioselective Synthesis of (R)-(-)-Carnitine from Glycerol
Marzi, Mauro,Minetti, Patrizia,Moretti, Giampiero,Tinti, Maria Ornella,De Angelis, Francesco
, p. 6766 - 6769 (2007/10/03)
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