Tandem One-pot Synthesis of Polysubstituted 1,3-Thiazine Derivatives  

作　　者：王树良 王翔 屠蔓苏 姜波 屠树江 

机构地区：[1]Jiangsu Key Laboratory of Green Synthetic Chemistry for Functional Materials, School of Chemistry and Chemical Engineering, Xuzhou Normal University, Xuzhou, Jiangsu 221116, China

出　　处：《Chinese Journal of Chemistry》2011年第11期2411-2415,共5页中国化学（英文版）

基　　金：Project supported by the National Natural Science Foundationof China （Nos. 21072163, 21002083 and 21110102002）, the Science Foundation in Interdisciplinary Major Research Project of Xuzhou Normal University （No. 09XKXK01）, the Priority Academic Program Development of Jiangsu Higher Education Institutions, and the Doctoral Research Foundation of Xuzhou Normal University （No. 10XLR20）.

摘　　要：A tandem one-pot synthesis of polysubstituted 1,3-thiazines has been developed by reacting with cyanoacetamide and isothiocyanate derivatives to give rise to 2-cyano-3-mercaptoacrylamides, which are trapped in situ by various aldehydes or diversely substituted ketones through intermolecular cyclization, providing polysubstituted 1,3-thiazine derivatives in short reaction times with good to excellent yields. The salient features of this novel protocol are operational simplicity, accessing the desired products from the readily available starting materials and easy of product isolation and may find wide spread applications in medicinal chemistry.A tandem one-pot synthesis of polysubstituted 1,3-thiazines has been developed by reacting with cyanoacetamide and isothiocyanate derivatives to give rise to 2-cyano-3-mercaptoacrylamides, which are trapped in situ by various aldehydes or diversely substituted ketones through intermolecular cyclization, providing polysubstituted 1,3-thiazine derivatives in short reaction times with good to excellent yields. The salient features of this novel protocol are operational simplicity, accessing the desired products from the readily available starting materials and easy of product isolation and may find wide spread applications in medicinal chemistry.

关 键 词：one-pot synthesis polysubstituted 1 3-thiazines tandem reaction 

分 类 号：TQ457.29[化学工程—农药化工] O625[理学—有机化学]