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Tert ‐Butyl Nitrite Mediated Expeditious Methylsulfoxidation of Tetrazole‐amines with DMSO: Metal‐free Synthesis of Antifungal Active Methylsulfinyl‐1 H ‐tetrazole Derivatives
Author(s) -
Dai Peng,
Luo Kai,
Yu Xiang,
Yang WenChao,
Wu Lei,
Zhang WeiHua
Publication year - 2018
Publication title -
advanced synthesis and catalysis
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.541
H-Index - 155
eISSN - 1615-4169
pISSN - 1615-4150
DOI - 10.1002/adsc.201701364
Subject(s) - chemistry , tetrazole , antifungal , nitrite , combinatorial chemistry , selectivity , organic chemistry , medicinal chemistry , catalysis , nitrate , medicine , dermatology
A tert ‐butyl nitrite mediated methyl‐sulfoxidation of tetrazole‐amines in neat DMSO or methyl‐sulfinyl derivatives is revealed for the first time. The reaction exhibits good group tolerance, as well as highly selectivity to sulfinyl substitutions. This new protocol provides an expeditious and operationally simple procedure for C−S(O) bond construction. Preliminary bioactivity evaluation on selected products shows promising antifungal activities.