Palladium-catalyzed coupling of N-tosylhydrazones and β-bromostyrene derivatives: new approach to 2H-chromenes
作者:Yamu Xia、Ying Xia、Yan Zhang、Jianbo Wang
DOI:10.1039/c4ob01979b
日期:——
structural motif that exists in natural products and non-natural compounds possessing interesting biological activities. In this investigation, a highly efficient approach toward 2H-chromenes has been developed based on palladium-catalyzedcoupling of N-tosylhydrazones and β-bromostyrenes. The mechanism of this reaction is proposed that involves the formation of vinyl palladium by carbene migratory insertion
2 H -Chromene是存在于天然产物和具有有趣生物活性的非天然化合物中的重要结构基序。在这项研究中,基于钯催化的N-甲苯磺酰hydr和β-溴苯乙烯的偶联,已经开发出一种高效的2 H-苯甲基苯胺的方法。提出了该反应的机理,该机理涉及通过卡宾迁移插入和分子内亲核取代形成乙烯基钯。
Nickel-Catalyzed Cross-Coupling of Chromene Acetals and Boronic Acids
作者:Thomas J. A. Graham、Abigail G. Doyle
DOI:10.1021/ol300364s
日期:2012.3.16
nes is described. Under base-free conditions, readily accessible 2-ethoxy-2H-chromenes undergo Csp3–O activation and Csp3–C bond formation in the presence of an inexpensive nickel catalyst and boronicacids. This new strategy enables broad access to 2-substituted-2H-chromenes and has been applied to the late-stage incorporation of complex molecules, including the pharmaceuticals loratidine and indomethacin
描述了一种用于合成 2-芳基-和杂芳基-2 H-色烯的模块化和高效方案。在无碱条件下,容易获得的 2-乙氧基-2 H-色烯在廉价的镍催化剂和硼酸存在下经历 C sp 3 -O 活化和 C sp 3 -C 键形成。这种新策略可以广泛使用 2-取代-2 H-色烯,并已应用于复杂分子的后期掺入,包括药物氯雷他定和吲哚美辛甲酯。
Kinetic Resolution and Dynamic Kinetic Resolution of Chromene by Rhodium‐Catalyzed Asymmetric Hydroarylation
作者:Qingjing Yang、Yanbo Wang、Shihui Luo、Jun (Joelle) Wang
DOI:10.1002/anie.201900721
日期:2019.4.8
A highly efficient kineticresolution and dynamickineticresolution of chromene is reported for the first time and they procced by a rhodium‐catalyzed asymmetric hydroarylation pathway. This new approach offers versatile access to various chiral 2,3‐diaryl‐chromanes containing vicinal stereogenic centers, as well as the recovered chiral flavenes, in high yields with excellent ee values (s factor up
CHROMENE MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY
申请人:Bristol-Myers Squibb Company
公开号:US20140235672A1
公开(公告)日:2014-08-21
The present application describes modulators of MCP-1 or CCR-2 of formula
or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein W
1
, W
2
, W
3
, Y, Z, R
2
, R
3
, R
3′
and R
4
, are defined in the specification. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and transplant rejection using modulators of formula (I) are disclosed.
An unexpected rearrangement-hydration reaction sequence of 2H-chromenes to dihydrochalcones under catalysis of HAuCl4
作者:Gourhari Maiti、Utpal Kayal、Rajiv Karmakar、Rudraksha N. Bhattacharya
DOI:10.1016/j.tetlet.2012.08.117
日期:2012.11
2-Aryl-2H-chromenes in aqueous DCM medium under catalysis of HAuCl4 are converted into 3-(2-hydroxyaryl)-1-arylpropan-1-ones through hydration-rearrangement reaction sequence in very good yield. The key step probably involves the [1,5] hydride shift followed by the hydrolysis under the reaction condition. The notable advantages of this method are operational simplicity and ease of isolation of products and also provide a pathway to convert the chalcone into DHCs with the transposition of carbonyl group. (C) 2012 Elsevier Ltd. All rights reserved.