- Ruthenium-Catalyzed Vinylene Carbonate Annulation by C?H/N?H Functionalizations: Step-Economical Access to Indoles
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A convenient and effective method of ruthenium-catalyzed C?H/N?H annulations using vinylene carbonate as oxidizing acetylene surrogate has been disclosed. This method is scalable and compatible with a wide range of functional groups, providing a step-economical access to indole synthesis Preliminary mechanistic studies provided support for a reversible, acetate-assisted C?H ruthenation, along with a subsequent olefin insertion. (Figure presented.).
- Li, Bo,Li, Zheyu,Ma, Wenbo,Tan, Yuqiang,Wang, Yang,Yu, Yao,Zhang, Chunran,Zhao, Huan
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supporting information
(2022/01/11)
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- Na 2 CO 3-Catalyzed N-Acylation of Indoles with Alkenyl Carboxylates
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The N-acylation of indoles has been accomplished via inorganic base catalysis. It provided an efficient and simple catalysis system for the preparation of N-acylindoles with alkenyl carboxylates as acylating agents. A broad variety of indoles undergo the smooth N-acylation using Na 2 CO 3 as catalyst in MeCN at 120? °C to give the corresponding N-acylindoles in good to excellent yields.
- Zhou, Xiao-Yu,Chen, Xia
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supporting information
p. 516 - 521
(2019/01/10)
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- A indole compound and its preparation method and application (by machine translation)
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The invention discloses a indole compound and its preparation method and application. The indole compounds of the structural formula such as formula (I) is shown. The indoles, rice galenical demonstrate the excellent inhibitory activity, the effect of most of the compound is obviously better than the positive control drug validamycin; especially compound I - 43, I - 44, I - 54, I - 73, II - 7 and II - 17, its galenical very good living body protection and treating effect, effect is better than the positive control; more specifically, compound I - 43 of the rice sheath blight bacteriostatic activity than validamycin activity is improved by nearly 300 times. The indole compounds in the prevention and/or treatment of rice sheath blight has great application prospects. In addition the compound of the invention is simple in construction, the preparation method is simple, and is suitable for large-scale industrial production. (I). (by machine translation)
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Paragraph 0057; 0059
(2018/10/02)
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- A simple, effective, green method for the regioselective 3-acylation of unprotected indoles
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A fast and green method is developed for regioselective acylation of indoles in the 3-position without the need for protection of the NH position. The method is based on Friedel-Crafts acylation using acid anhydrides. The method has been optimized, and Y(OTf)3 in catalytic amounts is found to be the best catalyst together with the commercially available ionic liquid [BMI]BF4 (1-butyl-3-methylimidazolium tetrafluoro-borate) as solvent. The reaction is completed in a very short time using monomode microwave irradiation. The catalyst can be reused up to four times without significant loss of activity. A range of substituted indoles are investigated as substrates, and thirteen new compounds have been synthesized.
- Tran, Phuong Hoang,Tran, Hai Ngoc,Hansen, Poul Erik,Do, Mai Hoang Ngoc,Le, Thach Ngoc
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p. 19605 - 19619
(2015/11/27)
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- Palladium-catalyzed allylic alkylation of carboxylic acid derivatives: N-acyloxazolinones as ester enolate equivalents
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Triple A: A general asymmetric allylic alkylation of ester enolate equivalents at the carboxylic acid oxidation state is reported. N-Acylbenzoxazolinone-derived enol carbonates were synthesized and employed in the palladium-catalyzed alkylation reaction. The imide products were readily converted into a series of carboxylic acid derivatives without loss of enantiopurity.
- Trost, Barry M.,Michaelis, David J.,Charpentier, Julie,Xu, Jiayi
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supporting information; experimental part
p. 204 - 208
(2012/02/16)
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- Tandem copper-catalysed aryl and alkenyl amination reactions: The synthesis of N-functionalised indoles
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A Cu-diamine complex effectively catalyses tandem C-N bond formation on 2-(2-haloalkenyl)-aryl halide substrates, to deliver a series of N-functionalised indoles. Anilines, amides and carbamates are all effective coupling partners under the developed cond
- Hodgkinson, Roy C.,Schulz, Jurgen,Willis, Michael C.
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supporting information; experimental part
p. 432 - 434
(2009/06/28)
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- INDOLE SYNTHESES UTILIZING o-METHYLPHENYL ISOCYANIDES.
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New indole synthesis starting with o-methylphenyl isocyanides such as o-tolyl, 2,4-xylyl, and 2,6-xylyl isocyanide is described. Treatment of o-tolyl isocyanide with LDA in diglyme at minus 78 degree C generated selectively o-(lithiomethyl)phenyl isocyanide in an almost quantitative yield, which on warming up to room temperature was cyclized to indole after aqueous workup. Similarly, 2,4-xylyl and 2,6-xylyl and 2,6-xylyl isocyanides were cyclized to 5-methylindole and 7-methylindole quantitatively. The o-(lithiomethyl)phenyl isocyanides reacted with electrophiles such as alkyl halides and alkylene oxides to give o-alkylphenyl isocyanides, which were cyclized via the lithiation at the orthobenzylic carbon to afford 3-substituted indoles.
- Ito,Kobayashi,Seko,Saegusa
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