Based on the pseudo-dilution effect (PDE) on solid support, three cyclopeptides with an aliphatic-aryl ether bond as the bridge were synthesized via SN2 reaction between bromoacetylated at N-terminal and the phenol –...Based on the pseudo-dilution effect (PDE) on solid support, three cyclopeptides with an aliphatic-aryl ether bond as the bridge were synthesized via SN2 reaction between bromoacetylated at N-terminal and the phenol –OH group in C-terminal Tyr residue. All the products were obtained in good overall yields and characterized by related analytic data.展开更多
A novel facile solid-phase organic synthesis of aryl vinyl ethers by reaction of polystyrene-supported 2-phenylsulfonylethanol with phenols under Mitsunobu conditions and subsequent elimination reaction with DBU has b...A novel facile solid-phase organic synthesis of aryl vinyl ethers by reaction of polystyrene-supported 2-phenylsulfonylethanol with phenols under Mitsunobu conditions and subsequent elimination reaction with DBU has been developed. The advantages of this method include straightforward operation, good yield and high purity of the products. Alternatively, a typical example of Suzuki coupling reaction on-resin was further applied to prepare 4-phenylphenyl vinyl ether for extending this method.展开更多
This paper is a result of a review through 25 papers on the synthesis of three-, four-, five-, six-, and seven-membered rings on solid support. Solid-phase organic synthesis methods that enable the rapid production of...This paper is a result of a review through 25 papers on the synthesis of three-, four-, five-, six-, and seven-membered rings on solid support. Solid-phase organic synthesis methods that enable the rapid production of arrays of heterocycles are of critical importance to the pharmaceutical industry. The generation of heterocyclic chemistry by solid-phase synthesis will definitely accelerate the development of pharmaceutical research.展开更多
文摘Based on the pseudo-dilution effect (PDE) on solid support, three cyclopeptides with an aliphatic-aryl ether bond as the bridge were synthesized via SN2 reaction between bromoacetylated at N-terminal and the phenol –OH group in C-terminal Tyr residue. All the products were obtained in good overall yields and characterized by related analytic data.
基金Acknowledgement This work was supported by the National Natural Science Foundation of China （No. 21062007） and the Research Program of Jiangxi Province Department of Education （No. GJJ10385, GJJ11380）.
文摘A novel facile solid-phase organic synthesis of aryl vinyl ethers by reaction of polystyrene-supported 2-phenylsulfonylethanol with phenols under Mitsunobu conditions and subsequent elimination reaction with DBU has been developed. The advantages of this method include straightforward operation, good yield and high purity of the products. Alternatively, a typical example of Suzuki coupling reaction on-resin was further applied to prepare 4-phenylphenyl vinyl ether for extending this method.
文摘This paper is a result of a review through 25 papers on the synthesis of three-, four-, five-, six-, and seven-membered rings on solid support. Solid-phase organic synthesis methods that enable the rapid production of arrays of heterocycles are of critical importance to the pharmaceutical industry. The generation of heterocyclic chemistry by solid-phase synthesis will definitely accelerate the development of pharmaceutical research.
