Enol ethers as carbonyl surrogates in a modification of the Povarov synthesis of 3-aryl quinolines and their anti-Toxoplasma activity
作者:Carla E. Brown、James McNulty、Claudia Bordón、Robert Yolken、Lorraine Jones-Brando
DOI:10.1039/c6ob01083k
日期:——
A novel method for the preparation of 2-carboxyl-3-aryl quinoline derivatives from anilines, ethyl glyoxalate and enol ethers as phenylacetaldehyde surrogates is reported. The three-component coupling reaction occurs rapidly under mild conditions in dichloromethane catalysed by TFA. The method allows a more direct access to 3-aryl quinolines, sidestepping issues encountered with phenylacetaldehyde
An efficient racemic total synthesis of the bisbenzylisoquinoline alkaloids tetrandrine and isotetrandrine in four different routes is reported herein. Key steps of the synthesis include N-acyl Pictet-Spengler condensations to access the tetrahydroisoquinoline moieties, as well as copper-catalyzed Ullmann couplings for diaryl ether formation. Starting from commercially available building blocks tetrandrine
A transition-metal-free protocol for the synthesis of non-terminal alkenylethers, alkenylsulfides, and N-vinylazoles fromarylaldehydes or diarylketones, DMSO and O, S, N-nucleophiles has been reported. In this protocol, 24 examples of non-terminal alkenylethers and 28 examples of non-terminal alkenylsulfides in 72–95% yields have been synthesized within 5 min. Moreover, 27 examples of non-terminal
Methods of providing and using compounds having activity as inhibitors of cytochrome P450RAI
申请人:——
公开号:US20030078270A1
公开(公告)日:2003-04-24
Novel compounds having the Formulas 1 through 8, wherein the symbols have the meaning defined in the specification, and certain previously known compounds have been discovered to act as inhibitors of the cytochrome P450RAI (retinoic acid inducible) enzyme, and are used for treating diseases responsive to treatment by retinoids. The compound can also be used in co-treatment with retinoids.
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