Category: piperidines. In 2021 ANGEW CHEM INT EDIT published article about SUFEX CLICK CHEMISTRY; NUCLEOPHILIC-SUBSTITUTION; N-ALKYLATION; SULFONAMIDES; ARYL; DISCOVERY; AMINES; ARYLATION; PEPTIDES; REAGENTS in [Wei, Mingjie; Liang, Dacheng; Luo, Wenjun; Ma, Guojian; Liu, Zeyuan; Li, Le] Sun Yat Sen Univ, Sch Chem, PCFM Lab, Guangzhou 510275, Peoples R China; [Wei, Mingjie; Liang, Dacheng; Luo, Wenjun; Ma, Guojian; Liu, Zeyuan; Li, Le] Sun Yat Sen Univ, Sch Chem, GDHPRC Lab, Guangzhou 510275, Peoples R China; [Cao, Xiaohui] Guangdong Pharmaceut Univ, Sch Pharm, Guangzhou 510006, Peoples R China in 2021, Cited 144. The Name is 1,4-Dioxa-8-azaspiro[4.5]decane. Through research, I have a further understanding and discovery of 177-11-7.
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.
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Reference：
Piperidine – Wikipedia,
Piperidine | C5H7510N – PubChem