Selective electrophilic di- and monofluorinations for the synthesis of 4-difluoromethyl and 4-fluoromethyl quinazolin(thi)ones by a Selectfluor-triggered multi-component reaction  

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作  者:Ruiqin Zhang Renchao Ma Qinjiao Fu Rener Chen Zhiming Wang Lei Wang Yongmin Ma 

机构地区:[1]Institute of Advanced Studies and School of Pharmaceutical and Chemical Engineering,Taizhou University,Jiaojiang,Zhejiang,318000,P.R.China [2]School of Pharmaceutical Science,Zhejiang Chinese Medical University,Hangzhou,310053,P R China

出  处:《Organic Chemistry Frontiers》2022年第6期1567-1573,共7页有机化学前沿(英文)

基  金:supported by the Leading Innovative and Entrepreneur Team Introduction Program of Zhejiang(No.2019R01005).

摘  要:A simple and efficient domino protocol for the selective synthesis of 4-difluoromethyl and 4-fluoromethylquinazolin(thi)ones was established from readily available 2-aminoacetophenones and iso(thio)cyanatesmediated by Selectfluor. The reaction outcomes are restricted by the reaction environment. Without theuse of a base, gem-difluoro-oxylated quinazolin(thi)ones were afforded effectively as a sole product. Incontrast, only monofluoro-oxylated analogues were obtained under basic conditions.

关 键 词:conditions PRODUCT synthesis 

分 类 号:O62[理学—有机化学]

 

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