Water is found to be an efficient solvent for the Rh-catalyzed domino cyclization reaction of indoles with isoxazoles to yield indoloquinolines.

Abstract An efficient iron-catalyzed arylsulfonylation of activated alkenes has been developed. The protocol uses readily available N-acryl-N-substituted benzenesulfonamides and arylsulfinic acids as the starting materials, inexpensive iron salt as the catalyst, and environmentally friendly oxygen in air as the oxidant. α-Aryl-β-sulfonyl amides containing a quarternary stereocenter were obtained using N-acryl-N-alkyl benzenesulfonamides as the substrates.

AbstractA simple and efficient method for the arylsulfonylation of N‐acryl‐N‐substituted benzenesulfonamides with arylsulfonic acids is developed using environmentally friendly oxygen in air as the oxidant.

芳基上官能团的转化是化学领域中一个重要的研究方向,过渡金属催化芳环上的官能团转化取得了显著的成果.主要从过渡金属催化卤代芳烃、酚、芳胺、芳基叠氮、硝基苯衍生物、芳基硼酸酯的合成6个方面综述了过渡金属催化芳环上官能团转化的最新研究进展,并且展望了这些方法的应用前景,以期获得更加简单、高效、无毒的催化剂.

A convenient and efficient method for the copper-mediated cascade synthesis of diaryl sulfones via the Sandmeyer reaction has been developed. The protocol uses readily available aryl amines and arylsulfinic acids as the starting materials, isoamyl nitrite as the diazotizating reagent of the aryl amines, and the method shows mild reaction conditions and high tolerance towards various functional groups in the substrates.

A novel, simple and highly efficient method for the synthesis of 3-(trifluoromethyl)-indolin-2-one derivatives has been developed. The protocol uses readily available N-alkyl-N-phenylacrylamides as the starting materials, inexpensive and easily stored Langlois reagent (sodium trifluoromethanesulfinate) as the trifluoromethyl source, and iodobenzene diacetate [PhI(OAc)(2)] as the oxidant. The procedure involves a metal-free domino trifluoromethylation and arylation of alkenes. The methods did not need mediation of any transition metal which avoided contaminations of toxic metals in the products.

A simple and practical copper-catalyzed approach to oxindole derivatives by copper-catalyzed bis-arylation of N-alkyl-N-phenylacrylamides with diaryliodonium triflates has been developed under mild conditions, and the method is of tolerance towards some functional groups in the substrates.

An unexpected copper-catalyzed sequential C-arylation and denitrogenation of tetrazoles leading to 1,3-diaminoisoquinoline derivatives has been developed, and the corresponding 1,3-diaminoisoquinoline derivatives were obtained in moderate to good yields. The method provides a novel strategy for the synthesis of isoquinoline derivatives containing various functional groups.

An unexpected copper-catalyzed sequential C-arylation and denitrogenation of tetrazoles leading to 1,3-diaminoisoquinoline derivatives has been developed, and the corresponding 1,3-diaminoisoquinoline derivatives were obtained in moderate to good yields. The method provides a novel strategy for the synthesis of isoquinoline derivatives containing various functional groups.

Dicyclohexylphosphinic acid is synthesized via free radical addition reaction used diphenylphosphine and cyclohexene as the reagent,acetic acid as the solvent and di-t-butyl peroxide as the initiator,yielding 90%.The product is characterized by 1HNMR,13CNMR,31PNMR,ESI-MS.The advantages of this reaction are high yield,easy purification and mild condition.The free radical reaction mechanisms are suggested.

Carboxyl,amino,sulfhydryl derivatives of mPEG were synthesized starting from mPEG.The sructure of mPEG derivatives were confirmed by FT-IR,1HNMR and 13CNMR.

A series of telbivudine 3'-O-acetyl-5'-O-phenyl-N-alkylphosphramidate derivatives have been synthesized and their structures were confirmed by EI-MS,1H NMR and 13C NMR.We evaluated their anti-HBV activity in vitro.Two compounds 6d and 6f,turned out to be more active than telbivudine.

建立了一种新的保护的二糖半乳吡喃糖基（α1→2）葡萄吡喃糖苷的合成方法。甲基-4,6-O-苄叉基-β-D-葡萄吡喃糖苷（1）经区域选择性地苯甲酰化,得到受体甲基-3-O-苯甲酰基-4,6-O-苄叉基-β-D-葡萄吡喃糖苷（2）。该受体与供体异丙基-2-O-苯甲酰基-3-O-烯丙基-4,6-O-苄叉基-β-D-1-硫代半乳吡喃糖苷（4）偶联,获得了一种保护的二糖Galp（α1→2）Glcp片段甲基-2-O-苯甲酰基-3-O-烯丙基-4,6-O-苄叉基-α-D-半乳吡喃糖基-（1→2）-3-O-苯甲酰基-4,6-O-苄叉基-β-D-葡萄吡喃糖苷（5）。所有的产品通过NMR、MS等方法进行了结构表征。