An efficient synthesis of 4,5-diamino-3-halofuran-2（5H）-ones has been developed based on a sequential acylation and bisamination of mucohalic acids. The /5- and y-amination products have also been prepared with high...An efficient synthesis of 4,5-diamino-3-halofuran-2（5H）-ones has been developed based on a sequential acylation and bisamination of mucohalic acids. The /5- and y-amination products have also been prepared with high regioselectivity. This reaction shows some advantages in terms of its simple operation and readily available but highly functionalized starting material. All products gave satisfactory IR. 1H NMR. 13C NMR and HRMS.展开更多
The selective transalkylation of N-methyl tertiary amines with 3,4-dibromobutenolides is described. The N-methyl group of the parent tertiary amines was replaced by alkenyl units of the butenolides; and a series of bu...The selective transalkylation of N-methyl tertiary amines with 3,4-dibromobutenolides is described. The N-methyl group of the parent tertiary amines was replaced by alkenyl units of the butenolides; and a series of butenolide-containing tertiary enamines were obtained in moderate to good yields. Interestingly, the product 2b has shown a promising anticancer activity against HeLa cell lines （IC50 = 0.19μmol/L）.展开更多
基金support by the National Natural Science Foundation of China(No.21062014)the Key Project of Chinese Ministry of Education(No.210237)the Key Laboratory of Medicinal Chemistry for Natural Resource,Yunnan University(No. 200902205)
文摘An efficient synthesis of 4,5-diamino-3-halofuran-2（5H）-ones has been developed based on a sequential acylation and bisamination of mucohalic acids. The /5- and y-amination products have also been prepared with high regioselectivity. This reaction shows some advantages in terms of its simple operation and readily available but highly functionalized starting material. All products gave satisfactory IR. 1H NMR. 13C NMR and HRMS.
基金NSFC(No.21062014)the‘‘211’’Project in Ningxia University for financial support
文摘The selective transalkylation of N-methyl tertiary amines with 3,4-dibromobutenolides is described. The N-methyl group of the parent tertiary amines was replaced by alkenyl units of the butenolides; and a series of butenolide-containing tertiary enamines were obtained in moderate to good yields. Interestingly, the product 2b has shown a promising anticancer activity against HeLa cell lines （IC50 = 0.19μmol/L）.
