Indole synthesis: a review and proposed classification
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TL;DR: A framework for the classification of all indole syntheses is presented, and it is apparent that every indole synthesis must fit one or the other of the nine strategic approaches adumbrated here.
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About: This article is published in Tetrahedron. The article was published on 23 Sep 2011. and is currently open access. The article focuses on the topics: Indole test.
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Citations
Recent advances in organocatalytic methods for the synthesis of disubstituted 2- and 3-indolinones
TL;DR: This review aims to cover the literature on asymmetric quaternary carbons, 2-substituted and 2,2'-disubtituted 3-indolinones, from its origin to the end of 2011.
635
Indole synthesis – something old, something new
TL;DR: In this article, a general approach would start from a mono-functionalized arene such as an aniline or halobenzene, followed by cyclization with C-C or C-N bond formation to an unactivated C-H bond.
604
Indoles as therapeutics of interest in medicinal chemistry: Bird's eye view.
Navriti Chadha,Om Silakari +1 more
TL;DR: An overview of the chemistry, biology, and toxicology of indoles focusing on their application as drugs is provided to corroborate the information available on the natural indole alkaloids, indole based FDA approved drugs and clinical trial candidates having diverse therapeutic implementations.
516
Medicinal chemistry of indole derivatives: Current to future therapeutic prospectives.
Archana Kumari,Rajesh K. Singh +1 more
TL;DR: This review summarizes some of the recent effective chemical synthesis (2014-2018) for indole ring and emphasized on the structure-activity relationship (SAR) to reveal the active pharmacophores of various indole analogues accountable for anticancer, anticonvulsant, antimicrobial, antitubercular, antimalarial, antiviral, antidiabetic and other miscellaneous activities which have been investigated in the last five years.
427
Beyond C2 and C3: Transition-Metal-Catalyzed C–H Functionalization of Indole
TL;DR: This review focuses on the contributions made in benzenoid C–H functionalization of indoles and other related heteroaromatics such as carbazoles.
References
A new, general entry to 4-substituted indoles. Synthesis of (S)-(−)-pindolol and (±)-chuangxinmycin
Hiroyuki Ishibashi,Takashi Tabata,Kyoko Hanaoka,Hiroko Iriyama,Susumu Akamatsu,Masazumi Ikeda +5 more
TL;DR: In this article, a new method for synthesis of 4-substituted indoles has been developed by using the 7-arylthio-6-7-dihydroindol-4(5H) one5 as a common intermediate.
36
An improved synthesis of the unique anti-migraine agent cp-122,288 : a bromine atom passenger in an intramolecular heck reaction
TL;DR: In this paper, a 2,6-dibromoaniline was used in place of the original monobromo aniline in the indole forming intramolecular Heck reaction.
36
A new approach to the efficient indole synthesis by allene intramolecular cycloaddition
TL;DR: In this paper, a new development of efficient indole synthesis via allene intramolecular cycloaddition strategy is described, which is based on allene cyclo-cyclo-synthesis.
35
Synihesis of 3-substituied indoles via a modified madeling reaction
TL;DR: Anilides 4a-c,e-k, lla-d in which the amide function is benzylated, or silylated and having different electron-withdrawing groups (EWG) at the methyl methyl in the ortho position, cyclize under the influence of potassium tert-butoxide to the corresponding indole derivatives 5a,c, e-k and 9a-d, respectively as mentioned in this paper.
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A reinvestigation of 4-hydroxyindole-6-carboxylate synthesis from pyrrole-2-carboxaldehyde: A facile synthesis of indoles and indolizines
Musong Kim,Edwin Vedejs +1 more
TL;DR: Improved conditions for conversion to indoles 2, 5, and 6 are reported, and inconsistencies in some of the literature structure assignments and characterization data are noted.
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