Synthesis and relative binding affinity to steroid receptors and antiproliferative activity on MCF-7 cells of 2,3-disubstituted indenes
摘要:
The study of the relative binding affinity of a set of 2,3-disubstituted indenes to the receptors of steroid hormones indicates a weak effect of some derivatives on estrogen, progesterone and androgen receptors. The antiproliferative effect on human MCF-7 cells also shows a weak activity for three derivatives. (C) 1999 Elsevier Science S.A. All rights reserved.
[3,3]-Sigmatropic Rearrangement/5-<i>exo</i>-<i>dig</i> Cyclization Reactions of Benzyl Alkynyl Ethers: Synthesis of Substituted 2-Indanones and Indenes
作者:Armen A. Tudjarian、Thomas G. Minehan
DOI:10.1021/jo200271s
日期:2011.5.6
Substituted benzyl alkynyl ethers, prepared from the corresponding α-alkoxy ketones in a two-step sequence involving enol triflate formation and KOtBu-induced E2 elimination, undergo [3,3]-sigmatropic rearrangement/intramolecular 5-exo-dig cyclization at 60 °C to form substituted 2-indanones in good overall yields. 1,3-cis-Disubstituted-2-indanones are formed preferentially when the benzylic substituent
取代的苄基的炔醚,从在两步骤序列相应的α -烷氧基酮涉及烯醇三氟甲磺酸形成和KO制备吨卜诱导E2消除,经历[3,3] -sigmatropic重排/分子内-5-外-挖环化在60 °C 以良好的总产率形成取代的 2-茚满酮。当苄基取代基R 1较大时,1,3-顺式-二取代-2-茚满酮优先形成。取代的茚可以通过霍纳-沃兹沃思-埃蒙斯反应以高产率从 2-茚满酮制备。
Chemospecific Cyclizations of α‐Carbonyl Sulfoxonium Ylides on Aryls and Heteroaryls
作者:Daniel Clare、Benjamin C. Dobson、Phillip A. Inglesby、Christophe Aïssa
DOI:10.1002/anie.201910821
日期:2019.11.4
The functionalization of aryl and heteroaryls using α‐carbonylsulfoxoniumylides without the help of a directing group has remained so far a neglected area, despite the advantageous safety profile of sulfoxoniumylides. Described herein are the cyclizations of α‐carbonylsulfoxoniumylides onto benzenes, benzofurans and N‐p‐toluenesulfonyl indoles in the presence of a base in HFIP, whereas pyrroles
A Pd‐Catalyzed Annulation Strategy to Linearly Fused Functionalized N‐Heterocycles
作者:Larry Hoteite、Benjamin D. W. Allen、Ms. Ergaiya A. Elhajj、Anthony J. H. M. Meijer、Joseph P. A. Harrity
DOI:10.1002/chem.202400116
日期:2024.4.11
annulation strategy to linearly fused polycyclic piperidines from readily available substrates. These products can be chemoselectively functionalized to generate analogs that represent commonsubstructures in bioactive compounds.