title: A Neber approach for the synthesis of spiro-fused 2H-azirine-pyrazolone.
abstract: A base-mediated Neber reaction of enaminopyrazolones, which are the tautomers of 4-acyloxime-2-pyrazolin-5-ones, with sulfonyl chlorides was achieved. With this developed approach, a range of spiro-fused 2H-azirine-pyrazolones were obtained in good yields under mild conditions. A preliminary trial of a catalytic asymmetric version of the Neber reaction was conducted and gave promising enantioselectivity.
authors.affiliation: National Engineering Research Center of Chiral Drugs, Chengdu Institute of Organic Chemistry, Chinese Academy of Sciences, Chengdu 610041, China. xuxy@cioc.ac.cn yuanwc@cioc.ac.cn and University of Chinese Academy of Sciences, Beijing 100049, China.
authors.forename: Deng-Feng
authors.initials: DF
authors.lastname: Yue
authors.affiliation: National Engineering Research Center of Chiral Drugs, Chengdu Institute of Organic Chemistry, Chinese Academy of Sciences, Chengdu 610041, China. xuxy@cioc.ac.cn yuanwc@cioc.ac.cn and University of Chinese Academy of Sciences, Beijing 100049, China.
authors.forename: Jian-Qiang
authors.initials: JQ
authors.lastname: Zhao
authors.affiliation: National Engineering Research Center of Chiral Drugs, Chengdu Institute of Organic Chemistry, Chinese Academy of Sciences, Chengdu 610041, China. xuxy@cioc.ac.cn yuanwc@cioc.ac.cn and University of Chinese Academy of Sciences, Beijing 100049, China.
authors.forename: Zhen-Hua
authors.initials: ZH
authors.lastname: Wang
authors.affiliation: National Engineering Research Center of Chiral Drugs, Chengdu Institute of Organic Chemistry, Chinese Academy of Sciences, Chengdu 610041, China. xuxy@cioc.ac.cn yuanwc@cioc.ac.cn.
authors.forename: Xiao-Mei
authors.initials: XM
authors.lastname: Zhang
authors.affiliation: National Engineering Research Center of Chiral Drugs, Chengdu Institute of Organic Chemistry, Chinese Academy of Sciences, Chengdu 610041, China. xuxy@cioc.ac.cn yuanwc@cioc.ac.cn.
authors.forename: Xiao-Ying
authors.initials: XY
authors.lastname: Xu
authors.affiliation: National Engineering Research Center of Chiral Drugs, Chengdu Institute of Organic Chemistry, Chinese Academy of Sciences, Chengdu 610041, China. xuxy@cioc.ac.cn yuanwc@cioc.ac.cn.
authors.forename: Wei-Cheng
authors.initials: WC
authors.lastname: Yuan