Direct N‐Arylation of Azaheterocycles with Aryl Halides under Ligand‐free Condition

A simple and efficient C? N cross‐coupling method of aryl halides with various heterocycles was reported, by using 10 mol% of CuI as catalyst and 1.2 equiv. NaH as base. Aryl iodides, aryl bromides and many substituted aryl chlorides could efficiently react with heterocycles, providing variety of N‐arylated products in good to excellent yields. The ligand‐free catalyst system was stable in air and could be readily reused.     

无溶剂条件下方便、有效的方法合成3-氰基-2-吡啶酮衍生物

芳醛、丙酮和氰乙酰胺为原料,氢氧化钠为催化剂,在无溶剂条件下加热反应有效地合成2-吡啶酮衍生物,本方法具有反应时间短、条件温和、处理简单和环境友好等优点.     

Iridium-catalyzed enantioselective allylation of sodium 2-aminobenzenethiolate: an access to chiral benzo-fused N,S-heterocycles

The use of sodium 2-aminobenzenethiolate in the enantioselective iridium catalyzed allylic substitution with a range of methyl allyl carbonates allows the concise synthesis of the branch-type products with both excellent regio- and enantioselectivities, which are functionalized N,S-containing allylic intermediates for the formation of chiral benzo-fused N,S-heterocycles.     

An efficient Friedel-Crafts alkylation of nitrogen heterocycles catalyzed by antimony trichloride/montmorillonite K-10

It has been found that SbCl₃ supported on montmorillonite K-10 is an efficient and reusable catalyst for Friedel-Crafts alkylation of nitrogen heterocycles such as indoles and pyrroles with epoxides. The reaction gives the corresponding C-alkylated derivatives in good to excellent yields with a high regioselectivity.     

可见光促进的氧化还原催化反应在天然产物全合成中的应用

可见光促进的光氧化还原催化在近年来取得了重要进展, 许多可见光光氧化还原的反应被用于复杂分子的构建. 本文概述了这一领域的最新成果, 重点介绍该策略作为关键步骤在天然产物及类天然产物化合物的全合成中的应用.     

Synthesis of dihydropyrazolo[4,3-c]azepines via iodine-mediated intramolecular hydrative cyclization

A straightforward approach to substituted dihydropyrazolo[4,3-c]azepines via I₂-mediated intramolecular hydration in pyrazole-based allylamines prepared from Morita–Baylis–Hillman adducts of 4-iodopyrazolealdehyes is described.     

Synthesis of 5-(7-hydroxyhept-3-enyl)-1,2-dithiolan-3-one 1-oxide, a core functionality of antibiotic leinamycin

5-(7-Hydroxyhept-3-enyl)-1,2-dithiolan-3-one 1-oxide 1 possessing both the 1,2-dithiolan-3-one 1-oxide five-membered ring and the double bond at the gamma position of the heterocycle, characteristic of the antibiotic leinamycin, was synthesized. In addition, the activated ester form of 1 was prepared that may be useful for coupling 1 to certain DNA-binding agents.     

富勒烯[C60]杂环化合物的合成进展

综述了近年来通过环加成反应合成三元、五元、六元和七元杂环C₆₀衍生物的进展.     

Determining the scope of the lanthanide mediated, sequential hydroamination/C–C cyclization reaction: formation of tricyclic and tetracyclic aromatic nitrogen heterocycles

The scope of the lanthanide mediated, sequential hydroamination/C–C cyclization reaction was determined for the formation of tricyclic and tetracyclic aromatic nitrogen heterocycles. An array of ring sizes was explored to determine the diastereoselectivity. The electronic characteristics of the aromatic ring was also varied to determine how it affected the cascade reaction. It was found that the benzo[a]quinolizine and the pyrido[2,1,a]isoindolizine ring systems formed with the highest diastereoselectivity (>20:1), regardless of the electronic characteristics of the aromatic ring. Additionally, a tetracyclic indole nitrogen heterocycle was formed with a 2.3:1 diastereomeric ratio. A novel procedure for substrate preparation is also presented.