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Paper | Special issue | Vol 93, No. 2, 2016, pp.529-544
Published online, 26th November, 2015
DOI: 10.3987/COM-15-S(T)31
One-Pot Synthesis of Densely Functionalized Thiazoles and syn-3-Thioacrylates

Yi-Jing Dang, Mu-Yan Sun, Xiao-Yan Meng, Fu-Jie Zhao, Wen-Juan Hao, Bo Jiang, Shu-Jiang Tu, and Guigen Li*

*Department of Chemistry & Biochemistry, Texas Tech University, Lubbock, TX 79409-1061, U.S.A.


A sequential one-pot, two-step reaction has been established for ecient synthesis of densely functionalized thiazoles and syn-3-thioacrylates. Treatment of cyanoacetamide with isothiocyanates gave rise to 2-cyano-3-mercaptoacrylamides, trapped by but-2-ynedioates through [3+2] cyclization to access functionalized thiazoles. Using propiolates to replace but-2-ynedioates, the reaction resulted in highly substituted syn-3-thioacrylates. The present green synthesis shows several advantages including operational simplicity and fast reaction rates, which makes it a useful and attractive process of library generation for drug discovery.