Ring-opening 1,3-arylboration of arylcyclopropanes mediated by BCl<sub>3</sub>
作者:Yuichi Kuboki、Mitsuhiro Arisawa、Kenichi Murai
DOI:10.1039/d0ra08151e
日期:——
Herein, we report a ring-opening 1,3-arylboration of aryl cyclopropanes using BCl3 in the presence of arene nucleophiles. Formal 1,3-oxy arylation and 1,3-amino arylation of the arylcyclopropane via one-pot derivatization of the installed boron group were also achieved.
A facile approach for the synthesis of enantiopure γ-amino nitriles by copper-catalyzed aminocyanation of arylcyclopropanes is disclosed, which undergoes the highly enantioselective ring-opening reaction of cyclopropanes. The strategy utilizes N-fluorobenzenesulfonimide as nucleophilic nitrogen source as well as oxidant and trimethylsilyl cyanide as the other nucleophile, and it probably operates via
[EN] AMIDO COMPOUNDS AND THEIR USE AS PHARMACEUTICALS<br/>[FR] COMPOSÉS AMIDO ET LEUR UTILISATION COMME PRODUITS PHARMACEUTIQUES
申请人:INCYTE CORP
公开号:WO2005110992A1
公开(公告)日:2005-11-24
The present invention relates to inhibitors of 11-ß hydroxyl steroid dehydrogenase type 1, antagonists of the mineralocorticoid receptor (MR), and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11-ß hydroxyl steroid dehydrogenase type 1 and/or diseases associated with aldosterone excess.
Electrochemical‐induced 1,3‐oxohydroxylation of arylcyclopropanes
作者:Xuejin Huang、Jianhua Cai、Ye Zheng、Chunlan Song、Jiakun Li
DOI:10.1002/adsc.202301343
日期:2024.1.30
Herein, we present a method for electrochemical-induced 1,3-oxohydroxylation of arylcyclopropanes with H2O as the green oxygen source. This transformation offers a regioselective route to highly functionalized β-hydroxy ketones under oxidant- and metal-free conditions. Notably, this electrochemical approach features simple operation, good regioselectivity, high functional group tolerance, and easy
在此,我们提出了一种以 H 2 O 作为绿色氧源电化学诱导芳基环丙烷 1,3-氧代羟基化的方法。这种转化为在无氧化剂和无金属条件下制备高度功能化的β-羟基酮提供了一条区域选择性途径。值得注意的是,该电化学方法具有操作简单、区域选择性好、官能团耐受性高、产物易于衍生化等特点。机理研究提供了确凿的证据,证明 1,3-二醇是该反应中的关键中间体,导致观察到的区域选择性。
MOCHALOV S. S.; KARPOVA V. V.; SHABAROV YU. S., ZH. ORGAN. XIMII, 1980, 16, HO 10, 2092-2098