A new strategy for the chemoselective sulfonamide N-alkylation of sulfonyl ureas under neutral and mild conditions

An efficient and chemoselective sulfonamide N-alkylation of sulfonyl ureas is described. The sulfonyl urea derivatives, prepared in situ by the addition of an amine to an arylsulfonyl isocyanate, are selectively alkylated in excellent yields under neutral and mild conditions by treatment with trialkylphosphite-dimethyl acetylenedicarboxylate at ambient temperature.     

Copper(I)-catalyzed reaction of diaryl buta-1,3-diynes with cyclic amines: an atom-economic approach to amino-substituted naphthalene derivatives

1,4-Diaryl-1,3-butadiynes react with cyclic amines, such as pyrrolidine, piperidine, and morpholine in the presence of a catalytic amount of CuCl to afford amino-substituted naphthalene derivatives with good to high yields. The new catalytic procedure provides an atom-economic, one-pot synthetic method for the synthesis of naphthalene derivatives from easily available 1,4-diaryl-1,3-butadiynes.     

BF3·OEt2-catalyzed tandem Prins Friedel-Crafts reaction: a novel synthesis of sugar fused diarylhexahydro-2H-furo[3,2-b]pyrans

d-Glucose based homoallylic alcohol reacts smoothly with various aldehydes in the presence of arenes and a catalytic amount of BF₃·OEt₂ under mild conditions to afford a novel series of 5,7-diaryl-hexahydro-2H-furo[3,2-b]pyrans in good yields with high cis-selectivity.     

One-pot synthesis of aryl alkyl thioethers and diaryl disulfides using carbon disulfide as a sulfur surrogate in the presence of diethylamine catalyzed by copper(I) iodide in polyethylene glycol (PEG200)

A copper catalyzed one-pot protocol for the preparation of aryl alkyl thioethers and diaryl disulfides using carbon disulfide as the sulfur source and diethylamine in polyethylene glycol (PEG200) is described.     

Tris-(2-aminoethyl) amine as a novel and efficient tripod ligand for a copper(I)-catalyzed C-O coupling reaction

We have introduced a novel, efficient, commercially available and economically attractive N-donor tripod ligand, tris-(2-aminoethyl)amine for copper-catalyzed Ullmann diaryl ether synthesis. This catalyst system is highly active for both aryl iodides and aryl bromides. Variously substituted diaryl ethers have been synthesized in good to excellent yields.     

Addition of aryl cuprates to azides: a novel approach for the synthesis of unsymmetrical diaryl amines

Aryl and benzyl azides react smoothly with aryl cuprates, generated in situ from aryl magnesium bromide and CuCN in THF to furnish a variety of unsymmetrical diaryl amines in good yields. This is the first report on the synthesis of diarylamines from aryl azides and aryl bromides via an organometallic approach.     

Interaction of α,β-Unsaturated Ketones of the Adamantane Series with N,N'-Binucleophiles

The influence has been established of the structure of the initial ketone, the reactants, and the reaction conditions on the direction of the interaction of ,-unsaturated ketones of the adamantane series with hydrazine, phenylhydrazine, semicarbazide, thiosemicarbazide, urea, and thiourea. It was found that on interaction with hydrazine and phenylhydrazine both intermediate hydrazones and the final cyclization products, pyrazolines, were formed. Reaction with semicarbazide and thiosemicarbazide leads only to the synthesis of derivatives at the carbonyl group, semicarbazones and thiosemicarbazones, but with urea and thiourea leads to products of addition at the double bond.     

相转移催化法合成N，N＇－二芳基－1，4－苯二氧基二乙酰胺

于液－液相转移催化条件下，以ＰＥＧ－４００为催化剂，通过１，４－苯二氧基二乙酰氯与芳胺反应，合成了相应的酞胺３ａ～３０。     

抗艾滋病药物环尿素类化合物的结构表征及其生物活性的定量预测

提出一种新的结构描述子-按氢分类的电距矢量（H-MEDV），并用于环尿素类 化合物抗人类免疫缺陷病毒（human immuno-deficiency virus，简称HIV）活性预 测，籍以多元线性回归（MLR）建立了H-MEDV与活性之间的相关模型，取得了良好 的结果，相关系数达R = 0.971。另外采用逐步回归（SMR）从原模型参数中选取了 5个参数建立一新模型，其模型相关系数为R = 0.938；继以留一法（Leave-one- out，LOO）进行交互检验，相关系数与之接近，R = 0.908；说明了定量结构活性 相关模型具有很好的稳定性和预测能力。