An efficient dimedone-catalyzed synthesis of highly functionalized thiazol-2-yl substituted E-acrylonitrile derivatives has been established through two-step reaction of a-thiocyanate ketones with malononitrile and am...An efficient dimedone-catalyzed synthesis of highly functionalized thiazol-2-yl substituted E-acrylonitrile derivatives has been established through two-step reaction of a-thiocyanate ketones with malononitrile and amines. The a-thiocyanate ketones were subjected with malononitrile to provide thiazol-2-ylidenemalononitrile derivatives, followed with various amines in the presence of dimedone to yield the final thiazol-2-yl substituted acrylonitrile derivatives.展开更多
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...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.展开更多
基金Supporting information for this article is available On the WWW under http：Nd-xlcloi.orgi10. 1002/cjoc.201100719 or from the author.Acknowledgement We are grateful for financial support from the National Science Foundation of China （Nos. 21072163, 21102124）, PAPD of Jiangsu Higher Education Institutions, Jiangsu Science and Technology Support Program （No. BE2011045）, Science Foundation in Interdisciplinary Major Research Project of Xuzhou Normal University （No. 09XKXK01）, and the NSF of Jiangsu Education Committee （No. 11KJB 150016）.
文摘An efficient dimedone-catalyzed synthesis of highly functionalized thiazol-2-yl substituted E-acrylonitrile derivatives has been established through two-step reaction of a-thiocyanate ketones with malononitrile and amines. The a-thiocyanate ketones were subjected with malononitrile to provide thiazol-2-ylidenemalononitrile derivatives, followed with various amines in the presence of dimedone to yield the final thiazol-2-yl substituted acrylonitrile derivatives.
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）.
文摘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.
