Zang Qin, Zhou Aihua, Javed Salim, Maity Pradip K, Knudtson Chris A, Bi Danse, Hastings Jared J, Basha Fatima Z, Hanson Paul R
Department of Chemistry, University of Kansas, 1251 Wescoe Hall Drive, Lawrence, KS 66045-7582 and the University of Kansas Center for Chemical Methodologies and Library Development (KU-CMLD), 2034 Becker Drive, Delbert M. Shankel Structural Biology Center, Lawrence, Kansas 66047-3761.
Department of Chemistry, University of Kansas, 1251 Wescoe Hall Drive, Lawrence, KS 66045-7582 and the University of Kansas Center for Chemical Methodologies and Library Development (KU-CMLD), 2034 Becker Drive, Delbert M. Shankel Structural Biology Center, Lawrence, Kansas 66047-3761 ; H. E. J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Pakistan.
Heterocycles. 2012 Dec 31;86(2). doi: 10.3987/COM-12-S(N)121.
A novel one-pot sulfonylation/intramolecular thia-Michael protocol is reported for the synthesis of 1,5,2-dithiazepine 1,1-dioxides. Sulfonylation between cysteine ethyl ester/cysteamine and 2-chloroethanesulfonyl chloride, followed by intramolecular thia-Michael addition, was achieved and afforded the titled 1,5,2-dithiazepine-1,1-dioxide scaffolds. Diversification was demonstrated for future library synthesis.
报道了一种用于合成1,5,2-二噻氮杂卓1,1-二氧化物的新型一锅法磺酰化/分子内硫杂迈克尔反应。实现了半胱氨酸乙酯/半胱胺与2-氯乙烷磺酰氯之间的磺酰化反应，随后进行分子内硫杂迈克尔加成反应，得到了标题化合物1,5,2-二噻氮杂卓-1,1-二氧化物骨架。展示了用于未来文库合成的多样化方法。
